略歴
玉村 啓和(たまむら ひろかず)
Hirokazu Tamamura, Ph.D.
東京科学大学 総合研究院
生体材料工学研究所 メディシナルケミストリー分野
副学長/副研究院補佐/教授
博士(薬学)(京都大学)
〒101-0062 東京都千代田区神田駿河台 2-3-10
Tel: (03)5280-8036
Fax: (03)5280-8039
e-mail: tamamura.mr(ここに@をいれてください)tmd.ac.jp
生年月日
1964年7月24日
学歴・職歴・資格
1988年 京都大学薬学部卒業
1989年 京都大学大学院薬学研究科 修士課程 中退
1989-1997年 京都大学薬学部 助手
1997-2005年 京都大学大学院薬学研究科 講師、助教授
この間、
1999-2000年 米国国立がん研究所(National Cancer Institute/NIH) 博士研究員
2005年 東京医科歯科大学生体材料工学研究所 教授
2024年10月 東京工業大学との統合により、東京科学大学総合研究院生体材料工学研究所
副学長、副研究院長補佐、教授
専門
ペプチド・タンパク質化学、創薬化学、ケミカルバイオロジー
ペプチドミメティックを活用した中分子創薬、HIVやコロナウイルス等を対象とした抗ウイルス剤の創製に力を入れている。大学院生(1年しか在席していないが)の時から、アカデミックな創薬化学を基盤としながら、医薬品を開発したいと考えており、2023年にAphexdaTMがFDAより承認された。
所属学会
日本ケミカルバイオロジー研究会、日本薬学会、日本ペプチド学会、アメリカ化学会、日本エイズ学会、日本化学会、有機合成化学協会
受賞歴
- 2001年 日本薬学会奨励賞
- 1998年 第7回日本薬学会医薬化学部会年会ポスター賞
- 1998年 日本ペプチド学会奨励賞
List of publications of Hirokazu Tamamura, Ph. D.
- Kouki Shinohara, Takuya Kobayakawa, Kohei Tsuji, Yuki Takamatsu, Hiroaki Mitsuya & Hirokazu Tamamura
Naphthalen-1-ylethanamine–containing small molecule inhibitors of the papain-like protease of SARS-CoV-2.
Eur. J. Med. Chem., 280, 116963(article number) available online: Oct 18 (2024). doi: 10.1016/j.ejmech.2024.116963 (Science Tokyo press release) - Shin-ichiro Hattori, Haydar Bulut, Hironori Hayashi, Naoki Kishimoto, Nobutoki Takamune, Kazuya Hasegawa, Yuri Furusawa, Seiya Yamayoshi, Kazutaka Murayama, Hirokazu Tamamura, Mi Li, Alexander Wlodawer, Yoshihiro Kawaoka, Shogo Misumi & Hiroaki Mitsuya
Structural and virologic mechanism of the emergence of resistance to Mpro inhibitors in SARS-CoV-2.
Proc. Natl. Acad. Sci. USA, doi.org/10.1073/pnas.2404175121 - Kohei Tsuji, Hirokazu Tamamura & Terrence R. Burke, Jr.Application of a Fluorescence Recovery-based Polo-like Kinase 1 Binding Assay to Polo-like Kinase 2 and Polo-like Kinase 3.
Biol. Pharm. Bull., 47 (7), 1282-1287 (2024). doi.org/10.1248/bpb.b24-00189 (Featured Article) - Kohei Tsuji, Hirokazu Tamamura & Terrence R. Burke, Jr.Affinity enhancement of polo-like kinase 1 polo box domain-binding ligands by a bivalent approach using a covalent kinase-binding component.
RSC Chem. Biol., Online Publication Date: Jun 4 (2024). doi.org/10.1039/ d4cb00031e (Inside Front Cover, TMDU press release) - Takahiro Ishii, Takuya Kobayakawa, Kouki Matsuda, Kiyomi Nigorikawa, Peter Bolah, Airi Noborio, Kohei Tsuji, Nami Ohashi, Kazuhisa Yoshimura, Wataru Nomura, Hiroaki Mitsuya, Kenji Maeda & Hirokazu TamamuraDiscovery of Potent DAG-Lactone Derivatives as HIV Latency Reversing Agents
ACS Infect. Dis., 10 (6), 2250-2261 (2024). doi.org/10.1021/acsinfecdis.4c00194 (Supplementary Journal Cover, TMDU press release) - Takuya Kobayakawa, Hikaru Takano, Takahiro Ishii, Peter Bolah, Kohei Tsuji, Nami Ohashi, Wataru Nomura, Toshiaki Furuta & Hirokazu TamamuraEffect of two-photon excitation to 8-azacoumarin derivatives as photolabile protecting groups
Chem. Pharm. Bull., 72 (3), 311-312 (2024). doi.org/10.1248/cpb.c24-00013 (Featured Article) - Takuya Kobayakawa, Masaru Yokoyama, Kohei Tsuji, Sayaka Boku, Masaki Kurakami, Masayuki Fujino, Takahiro Ishii, Yutaro Miura, Soshi Nishimura, Kouki Shinohara, Kenichi Yamamoto, Peter Bolah, Osamu Kotani, Tsutomu Murakami, Hironori Sato & Hirokazu TamamuraDevelopment of small-molecule anti-HIV-1 agents targeting HIV-1 capsid proteins.
Chem. Pharm. Bull., 72 (1), 41-47 (2024). doi.org/10.1248/cpb.c23-00618 - Kohei Tsuji, Takuya Kobayakawa, Takahiro Ishii, Nobuyo Higashi-Kuwata, Chika Azuma, Kouki Shinohara, Yutaro Miura, Kenichi Yamamoto, Soshi Nishimura, Shin-ichiro Hattori, Haydar Bulut, Hiroaki Mitsuya & Hirokazu Tamamura
Exploratory Studies of Effective Inhibitors against the SARS-CoV-2 Main Protease by Halogen Incorporation and Amide Bond Replacement.
Chem. Pharm. Bull., 71, 879-886 (2023). - Kohei Tsuji, Takahiro Ishii, Takuya Kobayakawa, Nobuyo Higashi-Kuwata, Kouki Shinohara, Chika Azuma, Yutaro Miura, Hiroki Nakano, Naoya Wada, Shin-ichiro Hattori, Haydar Bulut, Hiroaki Mitsuya & Hirokazu Tamamura
Structure–Activity Relationship Studies of SARS-CoV-2 Main Protease Inhibitors Containing 4-Fluorobenzothiazole-2-carbonyl Moietie.
J. Med. Chem., 66, 13516-13529 (2023). doi.org/10.1021/acs.jmedchem.3c00777 (TMDU press release) - Takuya Kobayakawa, Masayuki Amano, Miyuki Nakayama, Kohei Tsuji, Takahiro Ishii, Yutaro Miura, Kouki Shinohara, Kenichi Yamamoto, Masao Matsuoka & Hirokazu Tamamura
Development of Anti-HBV Agents Targeting HBV Capsid Proteins.
RSC. Med. Chem., 14, 1973-1980 (2023). doi.org/10.1039/d3md00258f (TMDU press release) (Front Cover) - Takahiro Ishii, Takuya Kobayakawa, Kouki Matsuda, Kohei Tsuji, Nami Ohashi, Shingo Nakahata, Airi Noborio, Kazuhisa Yoshimura, Hiroaki Mitsuya, Kenji Maeda & Hirokazu Tamamura
Synthesis and evaluation of DAG-lactone derivatives with HIV-1 latency reversing activity.
Eur. J. Med. Chem., 256, 115449(article number) published: Aug 05 (2023). doi: 10.1016/j.ejmech.2023.115449 (TMDU press release, TMDU Int’l press release) - Kohei Tsuji, Kofi Baffour-Awuah Owusu, Yutaro Miura, Takahiro Ishii, Kouki Shinohara, Takuya Kobayakawa, Akino Emi, Takashi Nakano, Youichi Suzuki & Hirokazu Tamamura
Dimerized Fusion Inhibitor Peptides Targeting the HR1-HR2 Interaction of SARS-CoV-2.
RSC Adv., 13, 8779-8793 (2023). doi: 10.1039/d2ra07356k - Nobuyo Higashi-Kuwata, Kohei Tsuji, Hironori Hayashi, Haydar Bulut, Maki Kiso, Masaki Imai, Hiromi Ogata-Aoki, Takahiro Ishii, Takuya Kobayakawa, Kenta Nakano, Nobutoki Takamune, Naoki Kishimoto, Shin-ichiro Hattori, Debananda Das, Yukari Uemura, Yosuke Shimizu, Manabu Aoki, Kazuya Hasegawa, Satoshi Suzuki, Akie Nishiyama, Junji Saruwatari, Yukiko Shimizu, Yoshikazu Sukenaga, Yuki Takamatsu, Kiyoto Tsuchiya, Kenji Maeda, Kazuhisa Yoshimura, Shun Iida, Seiya Ozono, Tadaki Suzuki, Tadashi Okamura, Shogo Misumi, Yoshihiro Kawaoka, Hirokazu Tamamura & Hiroaki Mitsuya
Identification of SARS-CoV-2 Mpro inhibitors containing P1’ 4-fluorobenzothiazole moiety highly active against SARS-CoV-2. Nature Commun., 14, 1076(article number) (2023). doi: 10.1038/s41467-023-36729-0 - Takuya Kobayakawa, Masaru Yokoyama, Kohei Tsuji, Masayuki Fujino, Masaki Kurakami, Takato Onishi, Sayaka Boku, Takahiro Ishii, Yutaro Miura, Kouki Shinohara, Yuki Kishihara, Nami Ohashi, Osamu Kotani, Tsutomu Murakami, Hironori Sato & Hirokazu Tamamura
Low-molecular-weight Anti-HIV-1 Agents Targeting HIV-1 Capsid Proteins.
RSC Adv., 13, 2156-2167 (2023). doi: 10.1039/d2ra06837k - Kanako Matsuura, Mizuki Yamaura, Hiromi Sakawaki, Ai Himeno, Yalcin Pisil, Takuya Kobayakawa, Kohei Tsuji, Hirokazu Tamamura, Shuzo Matsushita & Tomoyuki MiuraSensitivity to a CD4 mimic of a consensus clone of monkey-adapted CCR5-tropic SHIV-MK38C.
Virology, 578, 171-179 (2023). doi.org/10.1016/j.virol.2022.12.004 - Haruki Kitamura, Sayaka Sukegawa, Kouki Matsuda, Kousuke Tanimoto, Takuya Kobayakawa, Kazuho Takahashi, Hirokazu Tamamura, Kiyoto Tsuchiya, Hiroyuki Gatanaga, Kenji Maeda & Hiroaki Takeuchi
4-Phenylquinoline-8-amine induces HIV-1 reactivation and apoptosis in latently HIV-1 infected cells.
Biochem. Biophys. Res. Commun., 641, 139-147 (2023). doi.org/10.1016/j.bbrc.2022.12.024 - Kaho Matsumoto, Takeo Kuwata, William Tolbert, Jonathan Richard, Shilei Ding, Jérémie Prévost, Shokichi Takahama, George Judicate, Takamasa Ueno, Hirotomo Nakata, Takuya Kobayakawa, Kohei Tsuji, Hirokazu Tamamura, Amos Smith III, Marzena Pazgier, Andrés Finzi & Shuzo Matsushita
Characterization of a novel CD4 mimetic compound YIR-821 against HIV-1 clinical isolates.
J. Virol., 97 (1), e01638-22 (2023). doi.org/10.1128/jvi.01638-22 - Rongyi Wang, Kohei Tsuji, Takuya Kobayakawa, Yishan Liu, Kazuhisa Yoshimura, Shuzo Matsushita, Shigeyoshi Harada & Hirokazu Tamamura
Hybrids of small CD4 mimics and gp41-related peptides as dual-target HIV entry inhibitors.
Bioorg. Med. Chem., 76, 117083(article number) (2022). doi.org: 10.1016/j.bmc.2022.117083 - Kohei Tsuji, Takahiro Ishii, Takuya Kobayakawa, Nobuyo Higashi-Kuwata, Chika Azuma, Miyuki Nakayama, Takato Onishi, Hiroki Nakano, Naoya Wada, Miki Hori, Kouki Shinohara, Yutaro Miura, Takuma Kawada, Hironori Hayashi, Shin-ichiro Hattori, Haydar Bulut, Debananda Das, Nobutoki Takamune, Naoki Kishimoto, Junji Saruwatari, Tadashi Okamura, Kenta Nakano, Shogo Misumi, Hiroaki Mitsuya & Hirokazu Tamamura
Potent and Biostable Inhibitors of the Main Protease of SARS-CoV-2.
iScience, 25 (11), 105365(article number) published: Nov 01 (2022). doi.org/10.1016/j.isci.2022.105365 (TMDU press release, TMDU Int’l press release) - Kohei Tsuji, David Hymel, Buyong Ma, Hirokazu Tamamura, Ruth Nussinovd & Terrence R. Burke, Jr.
Development of ultra-high affinity bivalent ligands targeting the polo-like kinase 1.
RSC Chemical Biology, 3 (9), 1111-1120 (2022). doi: 10.1039/D2CB00153E (Back Cover picture) - Kohei Tsuji, Takuya Kobayakawa, Kiju Konno, Ami Masuda, Kohei Takahashi, Nami Ohashi, Kazuhisa Yoshimura, Takeo Kuwata, Shuzo Matsushita, Shigeyoshi Harada & Hirokazu Tamamura
Exploratory Studies on Soluble Small Molecule CD4 Mimics as HIV Entry Inhibitors.
Bioorg. Med. Chem., 56, 116616(article number) (2022). doi.org: 10.1016/j.bmc.2022.116616 (Cover picture) - Kohei Tsuji, Takahiro Ishii, Takuya Kobayakawa, Nami Ohashi, Wataru Nomura, & Hirokazu Tamamura
Fluorescence Resonance Energy Transfer-based Screening for Protein Kinase C Ligands Using 6-Methoxynaphthalene-labeled 1,2-Diacylglycerol-lactones
Org. Biomol. Chem., 19(38), 8264-8271 (2021). doi: 10.1039/d1ob00814e (Inside Front Cover) - Takuya Kobayakawa, Chika Azuma, Yuki Watanabe, Shunsuke Sawamura, Atsuhiko Taniguchi, Yoshio Hayashi, Kohei Tsuji & Hirokazu Tamamura
Development of Methods for Convergent Synthesis of Chloroalkene Dipeptide Isosteres and Its Application
J. Org. Chem., 86(7), 5091-5101 (2021). doi.org: 10.1021/acs.joc.0c03019 (TMDU & TOYAKU press release) - Kouki Matsuda, Takuya Kobayakawa, Ryusho Kariya, Kiyoto Tsuchiya, Kohei Tsuji, Takahiro Ishii, Hiroyuki Gatanaga, Kazuhisa Yoshimura, Seiji Okada, Hiroaki Mitsuya, Hirokazu Tamamura & Kenji Maeda
A Therapeutic Strategy to Combat HIV-1 Latently Infected Cells with a Combination of Latency-reversing Agents Containing DAG-lactone PKC Activators
Frontiers in Microbiology, 2021 Mar 17;12:636276. doi: 10.3389/fmicb.2021.636276. eCollection 2021. - Jan Vincent V. Arafiles, Hisaaki Hirose, Yusuke Hirai, Masahi Kuriyama, Maxwell Mamfe Sakyiamah, Wataru Nomura, Kazuhiro Sonomura, Miki Imanishi, Akira Otaka, Hirokazu Tamamura & Shiroh Futaki
Discovery of a Macropinocytosis-inducing Peptide Potentiated by Medium-mediated Intramolecular Disulfide Formation
Angew. Chem., Int. Ed., 60(21), 11928-11936 (2021). doi: 10.1002/anie.202016754 - Takuya Kobayakawa, Masaru Yokoyama, Kohei Tsuji, Masayuki Fujino, Masaki Kurakami, Sayaka Boku, Miyuki Nakayama, Moemi Kaneko, Nami Ohashi, Osamu Kotani, Tsutomu Murakami, Hironori Sato & Hirokazu Tamamura
Small-molecule Anti-HIV-1 Agents Based on HIV-1 Capsid Proteins.
Biomolecules, 11, 208 (2021). https://doi.org/10.3390/biom11020208 (TMDU & AMED press release) - Takuya Kobayakawa, Kohei Tsuji, Kiju Konno, Ai Himeno, Ami Masuda, Tingting Yang, Kohei Takahashi, Yusuke Ishida, Nami Ohashi, Takeo Kuwata, Kaho Matsumoto, Kazuhisa Yoshimura, Hiromi Sakawaki, Tomoyuki Miura, Shigeyoshi Harada, Shuzo Matsushita & Hirokazu Tamamura
Hybrids of Small-Molecule CD4 Mimics with Polyethylene Glycol Units as HIV Entry Inhibitors.
J. Med. Chem., 64(3), 1481-1496 (2021). doi.org: 10.1021/acs.jmedchem.0c01153 (Supplementary Journal Cover, TMDU & AMED press release) - Kohei Tsuji, Rongyi Wang, Takuya Kobayakawa, Kofi Baffour-Awuah Owusu, Masayuki Fujino, Moemi Kaneko, Naoki Yamamoto, Tsutomu Murakami & Hirokazu Tamamura
Potent Leads Based on CA-19L, an Anti-HIV Active HIV-1 Capsid Fragment.
Bioorg. Med. Chem., 30, 115923 (2021). doi.org: 10.1016/j.bmc.2020.115923 (Cover picture) - Daisuke Matsumoto, Hirokazu Tamamura & Wataru Nomura
A Cell Cycle-dependent CRISPR-Cas9 Activation System Based on an Anti-CRISPR Protein Shows Improved Genome Editing Accuracy.
Communications Biology, 3, 1-10 (2020). doi: 10.1038/s42003-020-01340-2 - Takuya Kobayakawa, Kento Ebihara, Kohei Tsuji, Takuma Kawada, Masayuki Fujino, Yuzuna Honda, Nami Ohashi, Tsutomu Murakami & Hirokazu Tamamura
Bivalent HIV-1 Fusion Inhibitors Based on Peptidomimetics.
Bioorg. Med. Chem., 28(24), 115812 (2020). doi.org: 10.1016/j.bmc.2020.115812 - Takuya Kobayakawa, Hikaru Takano, Takahiro Ishii, Kohei Tsuji, Nami Ohashi, Wataru Nomura, Toshiaki Furuta & Hirokazu Tamamura
Synthesis of Hydrophilic Caged DAG-lactones for Chemical Biology Applications.
Org. Biomol. Chem., 18, 4217-4223 (2020). doi: 10.1039/d0ob00807a - Kohei Tsuji, Kofi Baffour-Awuah Owusu, Takuya Kobayakawa, Rongyi Wang, Masayuki Fujino, Moemi Kaneko, Naoki Yamamoto, Tsutomu Murakami & Hirokazu Tamamura
Exploratory Studies on CA-15L, an Anti-HIV Active HIV-1 Capsid Fragment.
Bioorg. Med. Chem., 28(11), 115488 (2020). doi.org: 10.1016/j.bmc.2020.115488 - Daisuke Matsumoto, Hirokazu Tamamura & Wataru Nomura
TALEN-Based Chemically Inducible, Dimerization-Dependent, Sequence-Specific Nucleases.
Biochemistry, 59(2), 197-204 (2020). doi: 10.1021/acs.biochem.9b00798 - Mohammad Mamun Alam, Takeo Kuwata, Kazuki Tanaka, Muntasir Alam, Shokichi Takahama, Kazuya Shimura, Masao Matsuoka, Natsuki Fukuda, Hiroshi Morioka, Hirokazu Tamamura & Shuzo Matsushita
Synergistic Inhibition of Cell-to-cell HIV-1 Infection by Combinations of Single Chain Variable Fragments and Fusion Inhibitors.
Biochem Biophys Rep., 20, (2019). Sep 21; doi: 10.1016/j.bbrep.2019.100687. eCollection 2019 Dec. - Takuya Kobayakawa, Kento Ebihara, Yuzuna Honda, Masayuki Fujino, Wataru Nomura, Naoki Yamamoto, Tsutomu Murakami & Hirokazu Tamamura
C34 Dimeric Derivatives Utilizing Disulfide Bridges as Novel HIV-1 Fusion Inhibitors.
ChemBioChem: Special Issue dedicated to the 10th IPS in Kyoto, 20(16) 2101-2108 (2019). doi: 10.1002/cbic.201900187 (Cover picture) - Maxwell M. Sakyiamah, Wataru Nomura, Takuya Kobayakawa & Hirokazu Tamamura
Development of a NanoBRET-based Sensitive Screening Method for CXCR4 Ligands.
Bioconjugate Chem., 30(5), 1442-1450 (2019). doi: 10.1021/acs.bioconjchem.9b00182 - Maxwell M. Sakyiamah, Takuya Kobayakawa, Masayuki Fujino, Makoto Konno, Tetsuo Narumi, Tomohiro Tanaka, Wataru Nomura, Naoki Yamamoto, Tsutomu Murakami & Hirokazu Tamamura
Design, Synthesis and Biological Evaluation of Low Molecular Weight CXCR4 Ligands.
Bioorg. Med. Chem.: Special Issue entitled “Strategic Basic Molecular Medicinal Chemistry,” 27(6), 1130-1138 (2019). doi.org/10.1016/j.bmc.2019.02.013 - Takuya Kobayakawa, Kiju Konno, Nami Ohashi, Kohei Takahashi, Ami Masuda, Kazuhisa Yoshimura, Shigeyoshi Harada & Hirokazu Tamamura
Soluble-type Small-molecule CD4 Mimics as HIV Entry Inhibitors.
Bioorg. Med. Chem. Lett., 29(5), 719-723 (2019). doi.org/10.1016/j.bmcl.2019.01.011 - Kouki Matsuda, Takuya Kobayakawa, Kiyoto Tsuchiya, Shin-ichiro Hattori, Wataru Nomura, Hiroyuki Gatanaga, Kazuhisa Yoshimura, Shinichi Oka, Yasuyuki Endo, Hirokazu Tamamura, Hiroaki Mitsuya & Kenji Maeda
Benzolactam-Related Compounds Promote Apoptosis Via Protein Kinase C-Induced HIV Latency Reversal.
J. Biol. Chem., 294(1), 116-129 (2019). doi: 10.1074/jbc.RA118.005798. - Akinobu Z. Suzuki, Ryota Sekine, Shiori Takeda, Ryosuke Aikawa, Yukiko Shiraishi, Tomomi Hamaguchi, Hiroyuki Okuno, Hirokazu Tamamura & Toshiaki Furuta
A Clickable Caging Group as a New Platform for Modular Caged Compounds with Improved Photochemical Properties.
Chem. Comm., 55, 451-454 (2019). doi: 10.1039/c8cc07981a - Wataru Nomura, Daisuke Matsumoto, Taisuke Sugii, Takuya Kobayakawa & Hirokazu Tamamura
Efficient and Orthogonal Transcription Regulation by Chemically Inducible Artificial Transcription Factors.
Biochemistry, 57(45), 6452-6459 (2018). doi: 10.1021/acs.biochem.8b00741 - Takuya Kobayakawa, Nami Ohashi, Yuki Hirota, Kohei Takahashi, Yuko Yamada, Tetsuo Narumi, Kazuhisa Yoshimura, Shuzo Matsushita, Shigeyoshi Harada & Hirokazu Tamamura
Flexibility of Small Molecular CD4 Mimics as HIV Entry Inhibitors.
Bioorg. Med. Chem., 26(21), 5664-5671 (2018). doi.org: 10.1016/j.bmc.2018.10.011 - Kei Toyama, Takuya Kobayakawa, Wataru Nomura & Hirokazu Tamamura
Inhibition of EGFR Activation by Bivalent Ligands Based on a Cyclic Peptide Mimicking the Dimerization Arm Structure of EGFR.
Chem. Pharm. Bull., 66(11), 1083-1089 (2018). - Kei Toyama, Wataru Nomura, Takuya Kobayakawa & Hirokazu Tamamura
Delivery of a Proapoptotic Peptide to EGFR-Positive Cancer Cells by a Cyclic Peptide Mimicking the Dimerization Arm Structure of EGFR.
Bioconjugate Chem., 29(6), 2050-2057 (2018). doi: 10.1021/acs.bioconjchem.8b00250 - Takuya Kobayakawa, Yudai Matsuzaki, Kentaro Hozumi, Wataru Nomura, Motoyoshi Nomizu & Hirokazu Tamamura
Synthesis of a Chloroalkene Dipeptide Isostere-Containing Peptidomimetic and Its Biological Application.
ACS Med. Chem. Lett., 9(1), 6-10 (2018). doi: 10.1021/acsmedchemlett.7b00234 - Nami Ohashi, Ryosuke Kobayashi, Wataru Nomura, Takuya Kobayakawa, Agnes Czikora, Brienna K Herold, Nancy E. Lewin, Peter M. Blumberg& Hirokazu Tamamura
Synthesis and Evaluation of Dimeric Derivatives of Diacylglycerol-Lactones as Protein Kinase C Ligands.
Bioconjugate Chem., 28(8), 2135-2144 (2017) - Takuya Kobayakawa & Hirokazu Tamamura
Stereoselective Synthesis of Xaa-Yaa Type (Z)-Chloroalkene Dipeptide Isosteres via Efficient Utilization of Organocopper Reagents Mediated Allylic Alkylation.
Tetrahedron, 73(30), 4464-4471 (2017) - Kazuya Kobayashi, Takaaki Mizuguchi, Yasunao Hattori, Naho Ohara, Ryunosuke Ninomiya, Mika Iida, Honami Ooe, Yukako Yamazaki, Minami Takata, Hirokazu Tamamura & Kenichi Akaji
Effects of Replacement and Addition of an Amino Acid Contained in a Cyclic Peptide Corresponding to a β-Hairpin Loop Sequence of Human EGF Receptor.
J. Pept. Sci., 23(7-8), 581-586 (2017) - Hikaru Takano, Tetsuo Narumi, Wataru Nomura, and Hirokazu Tamamura
Microwave-Assisted Synthesis of Azacoumarin Fluorophores and the Fluorescence Characterization.
J. Org. Chem., 82(5), 2739-2744 (2017) - Tomohiro Tanaka, Toru Aoki, Wataru Nomura, Hirokazu Tamamura
Bivalent 14-mer Peptide Ligands of CXCR4 with Polyproline Linkers with Anti-Chemotactic Activity against Jurkat Cells.
J. Pept. Sci., 23(7-8), 574-580 (2017) - Takaaki Mizuguchi, Nami Ohashi, Daichi Matsumoto, Chie Hashimoto, Wataru Nomura, Naoki Yamamoto, Tsutomu Murakami & Hirokazu Tamamura
Development of Anti-HIV Peptides Based on a Viral Capsid Protein.
Biopolymers: Peptide Science, 2017 Jan;108(1). doi: 10.1002/bip.22920 (2017) - Tomofumi Nakamura, Joseph R. Campbell, Amber R. Moore, Sachiko Otsu, Haruo Aikawa, Hirokazu Tamamura & Hiroaki Mitsuya
Cell-based Assay System to Assess Human Immunodeficiency Virus Type 1 Integrase Multimerization.
J. Virol. Methods, 236, 196-206 (2016) - Takuya Kobayakawa & Hirokazu Tamamura
Efficient Synthesis of Xaa-Gly Type (Z)-Chloroalkene Dipeptide Isosteres via Organocuprate Mediated Reduction.
Tetrahedron, 72(32), 4968-4971 (2016) - Kei Toyama, Takaaki Mizuguchi, Wataru Nomura & Hirokazu Tamamura
Functional Evaluation of Fluorescein-Labeled Derivatives of a Peptide Inhibitor of the EGF Receptor Dimerization.
Bioorg. Med. Chem., 24(16), 3406-3412 (2016) - Kenichi Hiramatsu & Hirokazu Tamamura
A Mild Method for the Direct Fluorination of Pyrroles by Using a Lipophilic Anionic Phase-Transfer Catalyst.
Eur. J. Org. Chem., 2016(21), 3491-3494 (2016) - Wataru Nomura, Takaaki Mizuguchi & Hirokazu Tamamura
Multimerized HIV-gp41-derived Peptides as Fusion Inhibitors and Vaccines.
Biopolymers: Peptide Science, 106(4), 622-628 (2016) - Aisha Abduelmula, Ruijin Huang, Qin Pu, Hirokazu Tamamura, Gabriela Morosan-Puopolo & Beate Brand-Saberi
SDF-1 Controls the Muscle and Blood Vessel Formation of the Somite.
Int. J. Dev. Biol., 60(1-2-3), 29-38 (2016) - Nami Ohashi, Shigeyoshi Harada, Takaaki Mizuguchi, Yu Irahara, Yuko Yamada, Misato Kotani, Wataru Nomura, Shuzo Matsushita, Kazuhisa Yoshimura & Hirokazu Tamamura
Small Molecular CD4 Mimics Containing Mono-cyclohexyl Moieties as HIV Entry Inhibitors.
ChemMedChem a joint special issue with ChemBioChem: Protein–Protein Interactions, 11(8), 940-946 (2016) - Takaaki Mizuguchi, Shigeyoshi Harada, Tomoyuki Miura, Nami Ohashi, Tetsuo Narumi, Hiromi Mori; Yu Irahara; Yuko Yamada; Wataru Nomura, Shuzo Matsushita, Kazuhisa Yoshimura & Hirokazu Tamamura
A Minimally Cytotoxic CD4 Mimic as an HIV Entry Inhibitor.
Bioorg. Med. Chem. Lett., 26(2), 397-400 (2016) - Hikaru Takano, Tetsuo, Narumi, Wataru Nomura, Toshiaki Furuta & Hirokazu Tamamura
Utilization of the Heavy Atom Effect for the Development of a Photosensitive 8-Azacoumarin-type Photolabile Protecting Group.
Org. Lett., 17(21), 5372-5375 (2015) - Wataru Nomura, Haruo Aikawa, Shohei Taketomi, Miho Tanabe, Takaaki Mizuguchi & Hirokazu Tamamura
Exploration of Labeling of Near Infrared Dyes on the Polyproline Linker for Bivalent-Type CXCR4 Ligands.
Bioorg. Med. Chem., 23(21), 6967-6973 (2015) - Wataru Nomura, Taisuke Koseki, Nami Ohashi, Takaaki Mizuguchi & Hirokazu Tamamura
Trivalent Lignds for CXCR4 Bearing Polyproline Linkers Show Specific Recognition for Cells with Increased CXCR4 Expression.
Org. Biomol. Chem., 13(32), 8734-8739 (2015) - Takaaki Mizuguchi, Nami Ohashi, Wataru Nomura, Mao Komoriya, Chie Hashimoto, Naoki Yamamoto, Tsutomu Murakami, &
Bioorg. Med. Chem., 23(15), 4423-4427 (2015)
Anti-HIV Screening for Cell-Penetrating Peptides Using Chloroquine and Identification of Anti-HIV Peptides Derived from Matrix Proteins. - Wataru Nomura, Nami Ohashi, Atsumi Mori &
An In-cell Fluorogenic Tag-probe System for Protein Dynamics Imaging Enabled by Cell-Penetrating Peptides.
Bioconjugate Chem., 26(6), 1080-1085 (2015) - Takuya Kobayakawa, Tetsuo Narumi &
Remote Stereoinduction in the Organocuprate-Mediated Allylic Alkylation of Allylic gem-Dichlorides: Highly Diastereoselective Synthesis of (Z)-Chloroalkene Dipeptide Isosteres.
Org. Lett., 17(10), 2302-2305 (2015) - Nami Ohashi, Wataru Nomura, Natsuki Minato &
Screening for Protein Kinase C Ligands Using Fluorescence Resonance Energy Transfer.
Chem. Pharm. Bull.,62(10), 1019-1025 (2014) - Maryna Masyuk, Aisha Abduelmula, Gabriela Morosan-Puopolo, Veysel Odemis, Rizwan Rehimi, Nargis Khalida, Faisal Yusuf, Jurgen Engele,
Retrograde Migration of Pectoral Girdle Muscle Precursors Depends on CXCR4/SDF-1 Signaling.
Histochem. Cell. Biol.,142(5), 473-488 (2014)
, Carsten Theiss & Beate Brand-Saberi - Jun Yamamoto, Nami Maeda, Chiaki Komiya, Tomohiro Tanaka, Masaya Denda, Koji Ebisuno, Wataru Nomura,
Development of a Fluoride-responsive Amide Bond Cleavage Device that is Potentially Applicable to a Traceable Linker.
Tetrahedron, 70(34), 5122-5127 (2014)
, Youichi Sato, Aiko Yamauchi, Akira Shigenaga & Akira Otaka - Hikaru Takano, Tetsuo Narumi, Nami Ohashi, Akinobu Suzuki, Toshiaki Furuta, Wataru Nomura &
Development of the 8-Aza-3-bromo-7-hydroxycoumarin-4-ylmethyl Group as a New Entry of Photolabile Protecting Groups.
Tetrahedron, 70(29), 4400-4404 (2014) - Jun Yamamoto, Masaya Denda, Nami Maeda, Miku Kita, Chiaki Komiya, Tomohiro Tanaka, Wataru Nomura,
Development of a Traceable Linker Containing a Thiol-responsive Amino Acid for the Enrichment and Selective Labelling of Target Proteins.
Org. Biomol. Chem., 12(23), 3821-3826 (2014)
, Youichi Sato, Aiko Yamauchi, Akira Shigenaga & Akira Otaka - Tetsuo Narumi, Seiji Tsuzuki &
Imidazolium Salt-Catalyzed Friedel-Crafts-Type Conjugate Addition of Indoles: Analysis of Indole/Imidazolium Complex by High Level ab Initio Calculations.
Asian J. Org. Chem., 3(4), 497-503 (2014) - Tetsuo Narumi, Hikaru Takano, Nami Ohashi, Akinobu Suzuki, Toshiaki Furuta &
Isostere-Based Design of 8-Azacoumarin-Type Photolabile Protecting Groups: A Hydrophilicity Increasing Strategy for Coumarin-4-ylmethyls.
Org. Lett., 16(4), 1184-1187 (2014) - Nami Ohashi, Wataru Nomura, Tetsuo Narumi &
Peptide-based Ligand Screening and Functional Analysis of Protein Kinase C.
Biopolymers: Peptide Science, 100(6), 613-620 (2013) - Chie Hashimoto, Tetsuo Narumi, Hiroyuki Otsuki, Yuki Hirota, Hiroshi Arai, Kazuhisa Yoshimura, Shigeyoshi Harada, Nami Ohashi, Wataru Nomura, Tomoyuki Miura, Tatsuhiko Igarashi, Shuzo Matsushita &
A CD4 Mimic as an HIV Entry Inhibitor: Pharmacokinetics.
Bioorg. Med. Chem., 21(24), 7884-7889 (2013) - Chie Hashimoto, Wataru Nomura, Tetsuo Narumi, Masayuki Fujino, Toru Nakahara, Naoki Yamamoto, Tsutomu Murakami &
CXCR4-derived Synthetic Peptides Inducing Anti-HIV-1 Antibodies.
Bioorg. Med. Chem., 21(22), 6878-6885 (2013) - Hiroyuki Otsuki, Takayuki Hishiki, Tomoyuki Miura, Chie Hashimoto, Tetsuo Narumi,
Generation of a Replication-competent Simian-human Immunodeficiency Virus, the Neutralisation Sensitivity of Which can be Enhanced in the Presence of a Small Molecule CD4 Mimic.
J. Gen.Virol., 94(12), 2710-2716 (2013)
, Kazuhisa Yoshimura, Shuzo Matsushita & Tatsuhiko Igarashi - Chie Hashimoto, Wataru Nomura, Tetsuo Narumi, Masayuki Fujino, Hiroshi Tsutsumi, Masaki Haseyama, Naoki Yamamoto, Tsutomu Murakami &
Anti-HIV-1 Peptide Derivatives Based on the HIV-1 Co-receptor CXCR4.
ChemMedChem, 8(10), 1668-1672 (2013) - Wataru Nomura, Haruo Aikawa, Nami Ohashi, Emiko Urano, Mathieu Metifiot, Masayuki Fujino, Kasthuraiah Maddali, Taro Ozaki, Ami Nozue, Tetsuo Narumi, Chie Hashimoto, Tomohiro Tanaka, Yves Pommier, Naoki Yamamoto, Jun Komano, Tsutomu Murakami &
Cell-Permeable Stapled Peptides Based on HIV-1 Integrase Inhibitors Derived from HIV-1 Gene Products.
ACS Chem. Biol., 8(10), 2235-2244 (2013) - Wataru Nomura, Chie Hashimoto, Takaharu Suzuki, Nami Ohashi, Masayuki Fujino, Tsutomu Murakami, Naoki Yamamoto &
Multimerized CHR-derived Peptides as HIV-1 Fusion Inhibitors.
Bioorg. Med. Chem., 21(15), 4452-4458 (2013) - Tetsuo Narumi, Hiroshi Arai, Kazuhisa Yoshimura, Shigeyoshi Harada, Yuki Hirota, Nami Ohashi, Chie Hashimoto, Wataru Nomura, Shuzo Matsushita &
CD4 Mimics as HIV Entry Inhibitors: Lead Optimization Studies of the Aromatic Substituents.
Bioorg. Med. Chem., 21(9), 2518-2526 (2013) - Tetsuo Narumi, Haruo Aikawa, Tomohiro Tanaka, Chie Hashimoto, Nami Ohashi, Wataru Nomura, Takuya Kobayakawa, Hikaru Takano, Yuki Hirota, Tsutomu Murakami, Naoki Yamamoto &
Low Molecular Weight CXCR4 Ligands with Variable Spacers.
ChemMedChem, 8(1), 118-124 (2013) - Tetsuo Narumi, Takuya Kobayakawa, Haruo Aikawa, Shunsuke Seike &
Stereoselective Formation of Trisubstituted (Z)-Chloroalkenes Adjacent to a Tertiary Carbon Stereogenic Center by Organocuprate-Mediated Reduction/Alkylation.
Org. Lett., 14, 4490-4493 (2012) - Tetsuo Narumi, Tomohiro Tanaka, Chie Hashimoto, Wataru Nomura, Haruo Aikawa, Akira Sohma, Kyoko Itotani, Miyako Kawamata, Tsutomu Murakami, Naoki Yamamoto &
Pharmacophore-based small molecule CXCR4 ligands.
Bioorg. Med. Chem. Lett., 22, 4169-4172 (2012) - Chie Hashimoto, Wataru Nomura, Aki Ohya, Emiko Urano, Kosuke Miyauchi, Tetsuo Narumi, Haruo Aikawa, Jun A. Komano, Naoki Yamamoto &
Evaluation of a Synthetic C34 Trimer of HIV-1 gp41 as AIDS Vaccines.
Bioorg. Med. Chem., 20, 3287-3291 (2012) - Wataru Nomura, Akemi Masuda, Kenji Ohba, Arisa Urabe, Nobutoshi Ito, Akihide Ryo, Naoki Yamamoto &
Effects of DNA Binding of Zinc Finger and Linkers for Domain Fusion on Catalytic Activity of Sequence-Specific Chimeric Recombinases Determined by a Facile Fluorescent System.
Biochemistry, 51, 1510-1517(2012) - Wataru Nomura, Chie Hashimoto, Aki Ohya, Kosuke Miyauchi, Emiko Urano, Tomohiro Tanaka, Tetsuo Narumi, Toru Nakahara, Jun Komano, Naoki Yamamoto &
A Synthetic C34 Trimer of HIV-1 gp41 Shows Significant Increase of Inhibition Potency.
ChemMedChem, 7, 205-208 (2012) - Tetsuo Narumi, Mao Komoriya, Chie Hashimoto, Honggui Wu, Wataru Nomura, Shintaro Suzuki, Tomohiro Tanaka, Joe Chiba, Naoki Yamamoto, Tsutomu Murakami &
Conjugation of Cell-penetrating Peptides Leads to Identification of Anti-HIV Peptides from Matrix Proteins.
Bioorg. Med. Chem., 20, 1468-1474 (2012) - Tetsuo Narumi, Hiroshi Arai, Kazuhisa Yoshimura, Shigeyoshi Harada, Wataru Nomura, Shuzo Matsushita &
Small Molecular CD4 Mimics as HIV Entry Inhibitors.
Bioorg. Med. Chem., 19, 6735-6742 (2011) - Chie Hashimoto, Tomohiro Tanaka, Tetsuo Narumi, Wataru Nomura &
The Success and Failures of HIV Drug Discovery.
Expert Opin. Drug Discov., 6, 1067-1090 (2011) - Mitsuhiro Yamada, Hiroshi Kubo, Seiichi Kobayashi, Kota Ishizawa, Mei He, Takaya Suzuki, Naoya Fujino, Hiroyuki Kunishima, Masamitsu Hatta, Katsushi Nishimaki, Tetsuji Aoyagi, Kouichi Tokuda, Miho Kitagawa, Hisakazu Yano,
The Increase in Surface CXCR4 Expression on Lung Extravascular Neutrophils and its Effects on Neutrophils During Endotoxin-Induced Lung Injury.
Cell Mol. Immunol., 8, 305-314 (2011)
, Nobutaka Fujii & Mitsuo Kaku - Changshui Xu, Jianuo Liu, Lina Chen, Shangdong Liang, Nobutaka Fujii,
HIV-1 gp120 Enhances Outward Potassium Current via CXCR4 and cAMP-Dependent Protein Kinase a Signaling in Cultured Rat Microglia.
Glia., 59, 997-1007 (2011)
& Huangui Xiong - Wataru Nomura, Nami Ohashi, Yoshiaki Okuda, Tetsuo Narumi, Teikichi Ikura, Nobutoshi Ito &
Fluorescence-Quenching Screening of Protein Kinase C Ligands with an Environmentally Sensitive Fluorophore.
Bioconjugate Chem., 22, 923-930 (2011) - Tomohiro Tanaka, Tetsuo Narumi, Taro Ozaki, Akira Sohma, Nami Ohashi, Chie Hashimoto, Kyoko Itotani, Wataru Nomura, Tsutomu Murakami, Naoki Yamamoto &
Azamacrocyclic-metal Complexes as CXCR4 Antagonists.
ChemMedChem, 6, 834-839 (2011) - Hiroshi Tsutsumi, Seiichiro Abe, Tomoaki Mino, Wataru Nomura &
Intense Blue Fluorescence in a Leucine Zipper Assembly.
ChemBioChem, 12, 691-694 (2011) - Nami Ohashi, Wataru Nomura, Tetsuo Narumi, Nancy E. Lewin, Kyoko Itotani, Peter M. Blumberg &
Fluorescent-responsive Synthetic C1b Domains of Protein Kinase Cδ as Reporters of Specific High Affinity Ligand Binding.
Bioconjugate Chem., 22, 82-87 (2011) - Wataru Nomura, Tetsuo Narumi, Nami Ohashi, Yuki Serizawa, Nancy E. Lewin, Peter M. Blumberg, Toshiaki Furuta &
Synthetic Caged DAG-lactones for Photochemically-controlled Activation of Protein Kinase C.
ChemBioChem, 12, 535-539 (2011) - Tomohiro Tanaka, Wataru Nomura, Tetsuo Narumi, Akemi Masuda &
Bivalent Ligands of CXCR4 with Rigid Linkers for Elucidation of Dimerization State in Cells
J. Am. Chem. Soc.(Commun.),132, 15899-15901 (2010) - Tetsuo Narumi, Chihiro Ochiai, Kazuhisa Yoshimura, Shigeyoshi Harada, Tomohiro Tanaka, Wataru Nomura, Hiroshi Arai, Taro Ozaki, Nami Ohashi, Shuzo Matsushita &
CD4 Mimics Targeting the HIV Entry Mechanism and their Hybrid Molecules with a CXCR4 Antagonist
Bioorg. Med. Chem. Lett., 20, 5853-5858 (2010) - Shintaro Suzuki, Kasthuraiah Maddali, Chie Hashimoto, Emiko Urano, Nami Ohashi, Tomohiro Tanaka, Taro Ozaki, Hiroshi Arai, Hiroshi Tsutsumi, Tetsuo Narumi, Wataru Nomura, Naoki Yamamoto, Yves Pommier, Jun A. Komano &
Peptidic HIV Integrase Inhibitors Derived from HIV Gene Products: Structure-Activity Relationship Studies.
Bioorg. Med. Chem., 18, 6771-6775 (2010) - Shintaro Suzuki, Emiko Urano, Chie Hashimoto, Hiroshi Tsutsumi, Toru Nakahara, Tomohiro Tanaka, Yuta Nakanishi, Kasthuraiah Maddali, Yan Han, Makiko Hamatake, Kosuke Miyauchi, Yves Pommier, John A. Beutler, Wataru Sugiura, Hideyoshi Fuji, Tyuji Hoshino, Kyoko Itotani, Wataru Nomura, Tetsuo Narumi, Naoki Yamamoto, Jun A. Komano &
Peptide HIV-1 Integrase Inhibitors from HIV-1 Gene Products.
J. Med. Chem., 53(14), 5356-5360 (2010) - Kazuhisa Yoshimura, Shigeyoshi Harada, Junji Shibata, Makiko Hatada, Yuko Yamada, Chihiro Ochiai,
Enhanced Exposure of Human Immunodeficiency Virus Type 1 Primary Isolate Neutralization Epitopes through Binding of CD4 Mimetic Compounds.
J. Virol., 84(15), 7558-7568 (2010)
& Shuzo Matsushita - Toru Aoki, Saki Shimizu, Emiko Urano, Yuko Futahashi, Makiko Hamatake,
Improvement of Lentiviral Vector-mediated Gene Transduction by Genetic Engineering of the Structural Protein Pr55Gag.
Gene Ther., 17(9), 1124-1133(2010)
, Kazuo Terashima, Tsutomu Murakami, Naoki Yamamoto & Jun Komano - Roberta Melchionna, Anna Di Carlo, Roberta De Mori, Claudia Cappuzzello, Laura Barberi, Antonio Musar?, Chiara Cencioni, Nobutaka Fujii,
Induction of Myogenic Differentiation by SDF-1 via CXCR4 and CXCR7 Receptors.
Muscle Nerve., 41(6), 828-835 (2010)
, Marco Crescenzi, Maurizio C. Capogrossi, Monica Napolitano & Antonia Germani - Wataru Nomura, Tomoaki Mino, Tetsuo Narumi, Nami Ohashi, Akemi Masuda, Chie Hashimoto, Hiroshi Tsutsumi &
Development of Crosslink-Type Tag-Probe Pairs for Fluorescent Imaging of Proteins.
Biopolymers: Peptide Science, 94, 843-852 (2010) - Toru Nakahara, Wataru Nomura, Kenji Ohba, Aki Ohya, Tomohiro Tanaka, Chie Hashimoto, Tetsuo Narumi, Tsutomu Murakami, Naoki Yamamoto &
Remodeling of Dynamic Structures of HIV-1 Envelope Proteins Leads to Synthetic Antigen Molecules Inducing Neutralizing Antibodies.
Bioconjugate Chem., 21(4), 709-714 (2010) - Yuko Yamada, Chihiro Ochiai, Kazuhisa Yoshimura, Tomohiro Tanaka, Nami Ohashi, Tetsuo Narumi, Wataru Nomura, Shigeyoshi Harada, Shuzo Matsushita &
CD4 Mimics Targeting the Mechanism of HIV.
Bioorg. Med. Chem. Lett., 20, 354-358 (2010) - Hiroshi Tsutsumi, Wataru Nomura, Seiichiro Abe, Tomoaki Mino, Akemi Masuda, Nami Ohashi, Tomohiro Tanaka, Kenji Ohba, Naoki Yamamoto, Kazunari Akiyoshi &
Fluorogenically Active Leucine Zipper Peptides as New Tag-Probe Pairs for Protein Imaging in Living Cells.
Angew. Chem., Int. Ed., 48, 9164-9166 (2009) - Tomohiro Tanaka, Wataru Nomura, Tetsuo Narumi, Ai Esaka, Shinya Oishi, Nami Ohashi, Kyoko Itotani, Barry J. Evans, Zi-xuan Wang, Stephen C. Peiper, Nobutaka Fujii &
Structure-activity Relationship Study on Artificial CXCR4 Ligands Possessing the Cyclic Pentapeptide Scaffold: The Exploration of Amino Acid Residues of Pentapeptides by Substitutions of Several Aromatic Amino Acids.
Org. Biomol. Chem., 7, 3805-3809 (2009) - Nami Ohashi, Wataru Nomura, Mai Kato, Tetsuo Narumi, Nancy E. Lewin, Peter M. Blumberg &
Synthesis of Protein Kinase Cδ C1b Domain by Native Chemical Ligation Methodology and Characterization of Its Folding and Ligand Binding.
J. Pept. Sci., 5(10), 642-646 (2009) - Yuka Inaba, Nobuko Yoshimoto, Yuta Sakamaki, Makoto Nakabayashi, Teikichi Ikura,
A New Class of Vitamin D Analogues that Induce Structural Rearrangement of the Ligand-Binding Pocket of the Receptor.
J. Med. Chem., 52(5), 1438-1449 (2009)
, Nobutoshi Ito, Masato Shimizu & Keiko Yamamoto - Fuminori Mizukoshi, Kenji Baba, Yuko Goto-Koshino, Asuka Setoguchi-Mukai, Yasuhito Fujino, Koichi Ohno,
Inhibitory Effect of Newly Developed CXC-Chemokine Receptor 4 Antagonists on the Infection with Feline Immunodeficiency Virus.
J. Vet. Med. Sci., 71(1), 121-124 (2009)
, Shinya Oishi, Nobutaka Fujii & Hajime Tsujimoto - Tomohiro Tanaka, Hiroshi Tsutsumi, Wataru Nomura, Yasuaki Tanabe, Nami Ohashi, Ai Esaka, Chihiro Ochiai, Jun Sato, Kyoko Itotani, Tsutomu Murakami, Kenji Ohba, Naoki Yamamoto, Nobutaka Fujii &
Structure-activity Relationship Study of CXCR4 Antagonists Bearing the Cyclic Pentapeptide Scaffold: Identification of the New Pharmacophore.
Org. Biomol. Chem., 6, 4374-4377 (2008) - Wataru Nomura, Yasuaki Tanabe, Hiroshi Tsutsumi, Tomohiro Tanaka, Kenji Ohba, Naoki Yamamoto &
Fluorophore Labeling Enables Imaging and Evaluation of Specific CXCR4-Ligand Interaction at the Cell Membrane for Fluorescence-Based Screening.
Bioconjugate Chem., 19, 1917-1920 (2008)
A Future Perspective on the Development of Chemokine Receptor CXCR4 Antagonists.
Expert Opin. Drug Discov., 3(10), 1155-1166 (2008)
, Hiroshi Tsutsumi, Wataru Nomura, Tomohiro Tanaka & Nobutaka Fujii- Hirotomo Nakata, Seth M. Steinberg, Yasuhiro Koh, Kenji Maeda, Yoshikazu Takaoka,
Potent Synergistic Anti-Human Immunodeficiency Virus (HIV) Effects Using Combinations of the CCR5 Inhibitor Aplaviroc with Other Anti-HIV Drugs.
Antimicrob. Agents Chemother., 52(6), 2111-2119 (2008)
, Nobutaka Fujii & Hiroaki Mitsuya
Exploratory Studies on Development of the Chemokine Receptor CXCR4 Antagonists toward Downsizing.
Perspec. Medicin.l Chem., 2, 1-9 (2008)
, Hiroshi Tsutsumi, Wataru Nomura & Nobutaka Fujii- Wouter H. P., Driessen, Nobutaka Fujii,
Development of Peptide-targeted Lipoplexes to CXCR4-expressing Rat Glioma Cells and Rat Proliferating Endothelial Cells.
Mol. Ther., 16(3), 516-524 (2008)
& Sean M. Sullivan - Alexander Kasiyanov, Nobutaka Fujii,
Modulation of Network-driven, GABA-mediated Giant Depolarizing Potentials by SDF-1 in Developing Hippocampus.
Developmental Neuroscience, 30(4), 285-292 (2008)
& Huangui Xiong - Kenji Kabashima, Noriko Shiraishi, Kazunari Sugita, Tomoko Mori, Ayako Onoue, Miwa Kobayashi, Jun-ichi Sakabe, Ryutaro Yoshiki,
CXCL12-CXCR4 Engagement Is Required for Migration of Cutaneous Dendritic Cells.
Am. J Pathol., 171(4), 1249-1257 (2007)
, Nobutaka Fujii, Kayo Inaba & Yoshiki Tokura - Kenji Kabashima, Kazunari Sugita, Noriko Shiraishi,
CXCR4 Engagement Promotes Dendritic Cell Survival and Maturation.
Biochem. Biophys. Res. Commun., 361, 1012-1016 (2007)
, Nobutaka Fujii & Yoshiki Tokura
Versatile Use of Acid-catalyzed Ring-opening of β-Aziridinyl-α,β-enoates to Stereoselective Synthesis of Peptidomimetics.
Tetrahedron, 63, 9243-9254 (2007)
, Tomohiro Tanaka, Hiroshi Tsutsumi, Koji Nemoto, Satoko Mizokami, Nami Ohashi, Shinya Oishi & Nobutaka Fujii- Yamina A. Berchiche, Ken Y. Chow, Bernard Lagane, Martin Leduc, Yann Percherancier, Nobutaka Fujii,
Direct Assessment of CXCR4 Mutant Conformations Reveals Complex link between Receptor Structure and Galphai Activation.
J. Biol. Chem. (Commun.), 282, 5111 – 5115 (2007)
, Fran?oise Bachelerie & Nikolaus Heveker - Shiro Kubonishi, Tomoko Kikuchi, Shinya Yamaguchi,
Rapid Hematopoietic Progenitor Mobilization by Sulfated Colominic Acid.
Biochem. Biophys. Res. Commun., 355 (4), 970-975 (2007)
, Nobutaka Fujii, Takeshi Watanabe, Fernando Arenzana-Seisdedos, Kazuma Ikeda, Toshimitsu Matsui, Mitsune Tanimoto & Yoshio Katayama - Hiroshi Tsutsumi, Tomohiro Tanaka, Nami Ohashi, Hiroyuki Masuno,
Therapeutic Potential of the Chemokine Receptor CXCR4 Antagonists as Multi-functional Agents.
Biopolymers: Peptide Science, 88(2), 279-289 (2007)
, Kenichi Hiramatsu, Takanobu Araki, Satoshi Ueda, Shinya Oishi & Nobutaka Fujii - Satoshi Ueda, Shinya Oishi, Zi-xuan Wang, Takanobu Araki,
Structure-Activity Relationships of Cyclic Peptide-Based Chemokine Receptor CXCR4 Antagonists: Disclosing the Importance of Side-Chain and Backbone Functionalities.
J. Med. Chem., 50(2), 192-198 (2007)
, Jerome Cluzeau, Hiroaki Ohno, Shuichi Kusano, Hideki Nakashima, John O. Trent, Stephen C. Peiper & Nobutaka Fujii - Hiroshi Tsutsumi,
Inhibitors of the Chemokine Receptor CXCR4. Chemotherapy of AIDS, Metastatic Cancer, Leukemia and Rheumatoid Arthritis.
Lett. Drug Design Discovery, 4, 20-26 (2007)
& Nobutaka Fujii
Development of Low Molecular Weight CXCR4 Antagonists by Exploratory Structural Tuning of Cyclic Tetra- and Pentapeptide-scaffolds towards the Treatment of HIV Infection, Cancer Metastasis and Rheumatoid Arthritis.
Curr. Med. Chem., 14 (1), 93-102 (2007)
, Hiroshi Tsutsumi, Hiroyuki Masuno & Nobutaka Fujii- Ayumu Niida, Hiroaki Tanigaki, Eriko Inokuchi, Yoshikazu Sasaki, Shinya Oishi, Hiroaki Ohno,
Stereoselective Synthesis of 3,6-Disubstituted-3,6-dihydropyridin-2-ones as Potential Diketopiperazine Mimetics Using Organocopper-Mediated Anti-S(N)2 ‘ Reactions and Their Use in the Preparation of Low-Molecule CXCR4 Antagonists.
J. Org. Chem., 71 (10), 3942-3951 (2006)
, Zixuan Wang, Stephen C. Peiper, Kazuo Kitaura, Akira Otaka & Nobutaka Fujii
Development of a Linear Type of Low Molecular Weight CXCR4 Antagonists Based on T140 Analogs.
Org. Biomol. Chem., 4, 2354-2357 (2006)
, Hiroshi Tsutsumi, Hiroyuki Masuno, Satoko Mizokami, Kenichi Hiramatsu, Zixuan Wang, John O. Trent, Hideki Nakashima, Naoki Yamamoto, Stephen C. Peiper & Nobutaka Fujii
The Chemokine Receptor CXCR4 as a Therapeutic Target for Several Diseases.
Mini-Rev. Med. Chem., 6, 989-995 (2006)
, Hiroshi Tsutsumi & Nobutaka Fujii
Identification of a New Class of Low Molecular Weight Antagonists against the Chemokine Receptor CXCR4 Having the Dipicolylamine-Zinc(II) Complex Structure.
J. Med. Chem., 49 (11), 3412-3415 (2006)
, Akio Ojida, Teppei Ogawa, Hiroshi Tsutsumi, Hiroyuki Masuno, Hideki Nakashima, Naoki Yamamoto, Itaru Hamachi & Nobutaka Fujii- Eline Menu, Kewal Asosingh, Stefano Indraccolo, Hendrik De Raeve, Ivan Van Riet, Els Van Valckenborgh, Isabelle Vande Broek, Nobutaka Fujii,
The Involvement of Stromal Derived Factor 1α in Homing and Progression of Multiple Myeloma in the 5TMM Model.
Haematologica/the Hematology Journal, 91(5), 605-612 (2006)
, Ben Van Camp & Karin Vanderkerken - Hirofumi Hanaoka, Takahiro Mukai,
Development of a In-111-Labeled Peptide Derivative Targeting a Chemokine Receptor, CXCR4, for Imaging Tumors.
Nucl. Med. Biol., 33 (4), 489-494 (2006)
, Tomohiko Mori, Seigo Ishino, Kazuma Ogawa, Yasuhiko Iida, Ryuichiro Doi, Nobutaka Fujii & Hideo Saji - Alexander Kasyanov,
HIV-1 gp120 Enhances Giant Depolarizing Potentials via Chemokine Receptor CXCR4 in Neonatal Rat Hippocampus.
Eur. J. Neuroscience, 23, 1120-1128 (2006)
, Nobutaka Fujii & Huangui Xiong - Shinya Oishi, Kazuhide Miyamoto, Ayumu Niida, Mikio Yamamoto, Keiichi Ajito,
Application of Tri- and Tetrasubstituted Alkene Dipeptide Mimetics to Conformational Studies of Cyclic RGD Peptides.
Tetrahedron, 62, 1416-1424 (2006)
, Akira Otaka, Yoshihiro Kuroda, Akira Asai & Nobutaka Fujii
Specific Probes for Chemokine Receptors.
Chem. Biol., 13, 8-10 (2006)
& Hiroshi Tsutsumi- Ayumu Niida, Zixuan Wang, Kenji Tomita, Shinya Oishi,
Design and Synthesis of Downsized Metastin (45-54) Analogs with Maintenance of High GPR54 Agonistic Activity.
Bioorg. Med. Chem. Lett., 16(1), 134-137 (2006)
, Akira Otaka, Jean-Marc Navenot, James R. Broach, Stephen C. Peiper & Nobutaka Fujii
The Therapeutic Potential of CXCR4 Antagonists in the Treatment of HIV Infection, Cancer Metastasis and Rheumatoid Arthritis.
Expert Opin. Ther. Targets, 9 (6),1267-1282 (2005)
& Nobutaka Fujii
Structure-activity Relationship Studies on CXCR4 Antagonists Having Cyclic Pentapeptide Scaffolds.
Org. Biomol. Chem., 3, 4392-4394 (2005)
, Ai Esaka, Teppei Ogawa, Takanobu Araki, Satoshi Ueda, Zixuan Wang, John O. Trent, Hiroshi Tsutsumi, Hiroyuki Masuno, Hideki Nakashima, Naoki Yamamoto, Stephen C. Peiper, Akira Otaka & Nobutaka Fujii- Margitta Retz, Sachdev S. Sidhu, Jan Lehmann,
New HIV-Drug Inhibits in Vitro Bladder Cancer Migration and Invasion.
Eur. Urol., 48 (6), 1025-1030 (2005)
, Nobutaka Fujii & Carol Basbaum - Satoshi Ueda, Mizuno Fujita,
Photolabile Protection for One-Pot Sequential Native Chemical Ligation.
ChemBioChem, 6 (11), 1983-1986 (2005)
, Nobutaka Fujii & Akira Otaka - Jayendra B. Bhonsle, Zi-xuan Wang,
A Simple, Automated Quasi-4D-QSAR, Quasi-multi Way PLS Approach to Develop Highly Predictive QSAR Models for Highly Flexible CXCR4 Inhibitor Cyclic Peptide Ligands Using Scripted Common Molecular Modeling Tools.
QSAR Comb. Sci., 24 (5), 620-630 (2005)
, Nobutaka Fujii, Stephen C. Peiper & John O. Trent - Ayumu Niida, Shinya Oishi, Yoshikazu Sasaki, Makiko Mizumoto,
Facile Access to (Z)-Alkene-containing Diketopiperazine Mimetics Utilizing Organocopper-mediated Anti-SN2′ Reactions.
Tetrahedron Lett., 46, 4183-4186 (2005)
, Nobutaka Fujii & Akira Otaka - Meike Burger, Tanja Hartmann, Myriam Krome, Justyna Rawluk,
Small Peptide Inhibitors of the CXCR4 Chemokine Receptor (CD184) Antagonize the Activation, Migration and Antiapoptotic Responses of CXCL12 in Chronic Lymphocytic Leukemia B Cells.
Blood, 106 (5), 1824-1830 (2005)
, Nobutaka Fujii, Thomas J. Kipps & Jan A. Burger
Identification of Novel Low Molecular Weight CXCR4 Antagonists by Structural Tuning of Cyclic Tetrapeptide-scaffolds.
J. Med. Chem., 48, 3280-3289 (2005)
, Takanobu Araki, Satoshi Ueda, Zixuan Wang, Shinya Oishi, Ai Esaka, John O. Trent, Hideki Nakashima, Naoki Yamamoto, Stephen C. Peiper, Akira Otaka & Nobutaka Fujii- Yann Percherancier, Yamina Berchiche, Isabelle Slight, Rudolf Volkmer-Engert,
Bioluminescence Resonance Energy Transfer Reveals Ligand-induced Conformational Changes in CXCR4 Homo- and Heterodimers.
J. Biol. Chem., 280, 9895 – 9903 (2005)
, Nobutaka Fujii, Michel Bouvier & Nikolaus Heveker
Development of Anti-HIV Agents Targeting Dynamic Supramolecular Mechanism: Entry and Fusion Inhibitors Based on CXCR4/CCR5 Antagonists and gp41-C34-Remodeling Peptides.
Curr. HIV Res., 3 (4), 289 – 301 (2005)
, Akira Otaka & Nobutaka Fujii- Andrew C. W. Zannettino, Amanda N. Farrugia, Angela Kortesidis, Jim Manavis, Luen B. To, Sally K. Martin, Peter Diamond,
Elevated Serum Levels of SDF-1α are Associated with Increased Osteoclast Activity and Osteolytic Bone Disease in Multiple Myeloma Patients.
Cancer Res., 65(5), 1700-1709 (2005)
, Tsvee Lapidot, Nobutaka Fujii & Stan Gronthos - Daisuke Nameki, Eiichi Kodama, Mieko Ikeuchi, Naoto Mabuchi, Akira Otaka,
Mutations Conferring Resistance to HIV-1 Fusion Inhibitors Are Restricted by gp41 and Rev Responsive Element Functions.
J. Virol., 79, 764-770 (2005)
, Mutsuhito Ohno, Nobutaka Fujii & Masao Matsuoka
Stereoselective Synthesis of [L-Arg, L/D-3-(2-naphthyl)alanine]-Type (E)-Alkene Dipeptide Isosteres and its Application to the Synthesis and Biological Evaluation of Pseudopeptide Analogs of the CXCR4 Antagonist FC131.
J. Med. Chem., 48, 380-391 (2005)
, Kenichi Hiramatsu, Satoshi Ueda, Zixuan Wang, Shuichi Kusano, Shigemi Terakubo, John O. Trent, Stephen C. Peiper, Naoki Yamamoto, Hideki Nakashima, Akira Otaka & Nobutaka Fujii- Erich Piovan, Valeria Tosello, Stefano Indraccolo, Anna Cabrelle, Ilenia Baesso, Livio Trentin, Rita Zamarchi,
Chemokine Receptor Expression in EBV-associated Lymphoproliferation in Hu/SCID Mice: Implications for CXCL12/CXCR4 Axis in Lymphoma Generation.
Blood, 105, 931-939 (2005)
, Nobutaka Fujii, Gianpietro Semenzato, Luigi-Chieco Bianchi & Alberto Amadori - Christopher D. C. Allen, K. Mark Ansel, Caroline Low, Robin Lesley,
Germinal Center Dark and Light Zone Organization Is Mediated by CXCR4 and CXCR5.
Nat. Immunol., 5, 943-952 (2004)
, Nobutaka Fujii & Jason G. Cyster
Conformationally Constrained Analogues of Diacylglycerol (DAG). 23. Hydrophobic Ligand-Protein Interactions versus Ligand-Lipid Interactions of DAG-Lactones with Protein Kinase C (PK-C).
J. Med. Chem., 47, 4858-4864 (2004)
, Dina M. Sigano, Nancy E. Lewin, Megan L. Peach, Marc C. Nicklaus, Peter M. Blumberg & Victor E. Marquez- Akira Otaka, Satoshi Ueda, Kenji Tomita, Yoshiaki Yano,
Facile Synthesis of Membrane-embedded Peptides Utilizing Lipid Bilayer-assisted Chemical Ligation.
Chem. Commun., 2004 (15), 1722-1723 (2004)
, Katsumi Matsuzaki & Nobutaka Fujii
Identification of a CXCR4 Antagonist, a T140 Analog, as an Anti-rheumatoid Arthritis Agent.
FEBS Lett., 569 (1), 99-104 (2004)
, Miho Fujisawa, Kenichi Hiramatsu, Makiko Mizumoto, Hideki Nakashima, Naoki Yamamoto, Akira Otaka & Nobutaka Fujii- Mitsuko Takenaga,
A Single Treatment with Microcapsules Containing a CXCR4 Antagonist Suppresses Pulmonary Metastasis of Murine Melanoma.
Biochem. Biophys. Res. Commun., 320 (1), 226-232 (2004)
, Kenichi Hiramatsu, Natsumi Nakamura, Yoko Yamaguchi, Aki Kitagawa, Shinichi Kawai, Hideki Nakashima, Nobutaka Fujii & Rie Igarashi - Norio Yamamoto, Rongge Yang, Yoshiyuki Yoshinaka, Shinji Amari, Tatsuya Nakano, Jindrich Cinatl, Holger Rabenau, Hans Wilhelm Doerr, Gerhard Hunsmann, Akira Otaka,
HIV Protease Inhibitor Nelfinavir Inhibits Replication of SARS-associated Coronavirus.
Biochem. Biophys. Res. Commun., 318 (3), 719-725 (2004)
, Nobutaka Fujii & Naoki Yamamoto - Akira Otaka, Junko Watanabe, Akira Yukimasa, Yoshikazu Sasaki, Hideaki Watanabe, Takayoshi Kinoshita, Shinya Oishi,
SmI2-Mediated Reduction of γ,γ-Difluoro-α,β-enoates with Application to the Synthesis of Functionalized (Z)-Fluoroalkene-Type Dipeptide Isosteres.
J. Org. Chem., 69(5), 1634-1645 (2004)
& Nobutaka Fujii
Two Orthogonal Approaches to Overcome Multi-Drug Resistant HIV-1s: Development of Protease Inhibitors and Entry Inhibitors Based on CXCR4 Antagonists.
Curr. Drug Targets-Infectious Disorders, 4(2), 103-110 (2004)
& Nobutaka Fujii
Topochemical Exploration of Potent Compounds Using Retro-Enantiomer Libraries of Cyclic Pentapeptides.
Org. Biomol. Chem., 2, 1255-1257 (2004)
, Makiko Mizumoto, Kenichi Hiramatsu, Shuichi Kusano, Shigemi Terakubo, Naoki Yamamoto, John O. Trent, Zixuan Wang, Stephen C. Peiper, Hideki Nakashima, Akira Otaka & Nobutaka Fujii- Hui Peng, Yunlong Huang, Jeremy Rose, David Erichsen, Shelley Herek, Nobutaka Fujii,
Stromal Cell-Derived Factor 1-Mediated CXCR4 Signaling in Rat and Human Cortical Neural Progenitor Cells.
J. Neurosci. Res., 76, 35-50 (2004)
& Jialin Zheng
Conformationally Constrained Analogues of Diacylglycerol. 20. The Search for an Elusive Binding Site on Protein Kinase C (PK-C) through Relocation of the Carbonyl Pharmacophore along the sn-1 Side Chain of DAG-lactones.
J. Med. Chem., 47, 644-655 (2004)
, Dina M. Sigano, Nancy E. Lewin, Peter M. Blumberg & Victor E. Marquez- Tomohiko Mori, Ryuichiro Doi, Masayuki Koizumi, Eiji Toyoda, Daisuke Ito, Kazuhiro Kami, Toshihiko Masui, Koji Fujimoto,
CXCR4 Antagonist Inhibits Stromal Cell-derived Factor 1-induced Migration and Invasion of Human Pancreatic Cancer.
Mol. Cancer Ther., 3, 29-37 (2004)
, Kenichi Hiramatsu, Nobutaka Fujii & Masayuki Imamura - John O. Trent, Zi-xuan Wang, James L. Murray, Wenhai Shao,
Lipid Bilayer Simulations of CXCR4 with Inverse Agonists and Weak Partial Agonists.
J. Biol. Chem., 278, 47136-47144 (2003)
, Nobutaka Fujii & Stephen C. Peiper
Enhancement of the T140-based Pharmacophores Leads to the Development of More Potent and Bio-stable CXCR4 Antagonists.
Org. Biomol. Chem., 1, 3663-3669 (2003)
, Kenichi Hiramatsu, Makiko Mizumoto, Satoshi Ueda, Shuichi Kusano, Shigemi Terakubo, Miki Akamatsu, Naoki Yamamoto, John O. Trent, Zixuan Wang, Stephen C. Peiper, Hideki Nakashima, Akira Otaka & Nobutaka Fujii
Synthesis of Potent CXCR4 Inhibitors Possessing Low Cytotoxicity and Improved Biostability Based on T140 Derivatives.
Org. Biomol. Chem., 1, 3656-3662 (2003)
, Kenichi Hiramatsu, Shuichi Kusano, Shigemi Terakubo, Naoki Yamamoto, John O. Trent, Zixuan Wang, Stephen C. Peiper, Hideki Nakashima, Akira Otaka & Nobutaka Fujii
T140 Analogs as CXCR4 Antagonists Identified as Anti-metastatic Agents in the Treatment of Breast Cancer.
FEBS Lett., 550, 79-83 (2003)
, Akira Hori, Naoyuki Kanzaki, Kenichi Hiramatsu, Makiko Mizumoto, Hideki Nakashima, Naoki Yamamoto, Akira Otaka & Nobutaka Fujii- Toshina Oonuma, Masami Morimatsu, Takayuki Nakagawa, Rina Uyama, Nobuo Sasaki,
Role of CXCR4 and SDF-1 in Mammary Tumor Metastasis in the Cat.
J. Vet. Med. Sci., 65(10), 1069-1073 (2003)
, Nobutaka Fujii, Shizu Hashimoto, Hozumi Yamamura & Bunei Syuto - Nobutaka Fujii, Shinya Oishi, Kenichi Hiramatsu, Takanobu Araki, Satoshi Ueda,
Molecular-Size Reduction of a Potent CXCR4-Chemokine Antagonist Using Orthogonal Combination of Conformation- and Sequence-Based Libraries.
Angew. Chem. Int. Ed., 42(28), 3251-3253 (2003)
, Akira Otaka, Shuichi Kusano, Shigemi Terakubo, Hideki Nakashima, James A. Broach, John O. Trent, Zixuan Wang & Stephen C. Peiper
Synthesis of Potent -Secretase Inhibitors Containing a Hydroxyethylamine Dipeptide Isostere and Their Structure-Activity Relationship Studies.
Org. Biomol. Chem., 1(14), 2468-2473 (2003)
, Terukazu Kato, Akira Otaka & Nobutaka Fujii- Akira Otaka, Akira Yukimasa, Junko Watanabe, Yoshikazu Sasaki, Shinya Oishi,
Application of Samarium Diiodide (SmI2)-induced Reduction of γ-Acetoxy-α,β-enoates with α-Specific Kinetic Electrophilic Trapping for the Synthesis of Amino Acid Derivatives.
Chem. Commun., 2003(15), 1834-1835 (2003)
& Nobutaka Fujii - Tadashi Yasuda, A. Robin Poole, Makoto Shimizu, Takefumi Nakagawa, Sohel M. Julovi,
Involvement of CD44 in Induction of Matrix Metalloproteinases by a COOH-Terminal Heparin-Binding Fragment of Fibronectin in Human Articular Cartilage in Culture.
Arthritis Rheum., 48(5), 1271-1280 (2003)
, Nobutaka Fujii & Takashi Nakamura
Reduction of Peptide Character of HIV Protease Inhibitors that Exhibit Nanomolar Potency against Multi-drug Resistant HIV-1 Strains.
J. Med. Chem., 46(9), 1764-1768 (2003)
, Yasuhiro Koh, Satoshi Ueda, Yoshikazu Sasaki, Tomonori Yamasaki, Manabu Aoki, Kenji Maeda, Yoriko Watai, Hisashi Arikuni, Akira Otaka, Hiroaki Mitsuya & Nobutaka Fujii- Nobutaka Fujii, Hideki Nakashima &
The Therapeutic Potential of CXCR4 Antagonists in the Treatment of HIV.
Expert Opin. Investig. Drugs, 12(2), 185-195 (2003) - Shinya Oishi, Takae Kamano, Ayumu Niida, Yoshihiko Odagaki, Nobuyuki Hamanaka, Mikio Yamamoto, Keiichi Ajito,
Diastereoselective Synthesis of New ψ[(E)-CH=CMe]- and ψ[(Z)-CH=CMe]-type Alkene Dipeptide Isosteres by Organocopper Reagents and Application to Conformationally Restricted Cyclic RGD Peptidomimetics.
J. Org. Chem., 67(17), 6162-6173 (2002)
, Akira Otaka & Nobutaka Fujii - Akira Otaka, Fumihiko Katagiri, Takayoshi Kinoshita, Yoshihiko Odagaki, Shinya Oishi,
Regio- and Stereoselective Synthesis of (E)-Alkene trans-Xaa-Pro Dipeptide Mimetics Utilizing Organocopper-Mediated Anti-SN2′ Reactions.
J. Org. Chem., 67(17), 6152-6161 (2002)
, Nobuyuki Hamanaka & Nobutaka Fujii - Shinya Oishi, Ayumu Niida, Takae Kamano, Yoshihisa Miwa, Tooru Taga, Yoshihiko Odagaki, Nobuyuki Hamanaka, Mikio Yamamoto, Keiichi Ajito,
Regio- and Stereoselective Ring-opening of Chiral 1,3-Oxazolidin-2-one Derivatives by Organocopper Reagents Provides Novel Access to Di-, tri- and tetra-substituted Alkene Dipeptide Isosteres.
J. Chem. Soc., Perkin Trans. 1, 2002(15), 1786-1793 (2002)
, Akira Otaka & Nobutaka Fujii - Akira Otaka, Miki Nakamura, Daisuke Nameki, Eiichi Kodama, Susumu Uchiyama, Syota Nakamura, Hiroaki Nakano,
Remodeling of gp41-C34 Peptide Leads to Highly Effective Inhibitors of the Fusion of HIV-1 with Target Cells.
Angew. Chem. Int. Ed., 41(16), 2937-2940 (2002)
, Yuji Kobayashi, Masao Matsuoka & Nobutaka Fujii - Shinya Oishi, Ayumu Niida, Takae Kamano, Yoshihiko Odagaki,
Diastereoselective Synthesis of ψ[(E)-CH=CMe]- and ψ[(Z)-CH=CMe]-Type Dipeptide Isosteres Based on Organocopper-Mediated anti-SN2′ Reaction.
Org. Lett., 4(7), 1055-1058 (2002)
, Akira Otaka, Nobuyuki Hamanaka & Nobutaka Fujii - Shinya Oishi, Takae Kamano, Ayumu Niida, Yoshihiko Odagaki,
Diastereoselective Synthesis of ψ[(E)-CH=CMe]- and ψ[(Z)-CH=CMe]-Type Dipeptide Isosteres by Organocopper-Mediated anti-SN2′ Reaction.
Org. Lett., 4(7), 1051-1054 (2002)
, Akira Otaka, Nobuyuki Hamanaka & Nobutaka Fujii - Wen-bo Zhang, Jean-Marc Navenot, Bodduluri Haribabu,
A Point Mutation That Confers Constitutive Activity to CXCR4 Reveals T140 is an Inverse Agonist and AMD3100 and ALX40-4C Are Weak Partial Agonists.
J. Biol. Chem., 277(27), 24515-24521 (2002)
, Kenichi Hiramatsu, Akane Omagari, Gang Pei, Jhon P. Manfredi, Nobutaka Fujii, James R. Broach & Stephen C. Peiper
Synthesis and Evaluation of Pseudopeptide Analogs of a Specific CXCR4 Inhibitor, T140: The Insertion of an (E)-Alkene Dipeptide Isostere into the βII’-Turn Moiety.
Bioorg. Med. Chem. Lett., 12(6), 923-928 (2002)
, Kenichi Hiramatsu, Kazuhide Miyamoto, Akane Omagari, Shinya Oishi, Hideki Nakashima, Naoki Yamamoto, Yoshihiro Kuroda, Terumichi Nakagawa, Akira Otaka & Nobutaka Fujii
Certification of the Critical Importance of L-3-(2-Naphthyl)alanine at Position 3 of a Specific CXCR4 Inhibitor, T140, Leads to an Exploratory Performance of Its Downsizing Study.
Bioorg. Med. Chem., 10(5), 1417-1426 (2002)
, Akane Omagari, Kenichi Hiramatsu, Shinya Oishi, Hiromu Habashita, Taisei Kanamoto, Kazuyo Gotoh, Naoki Yamamoto, Hideki Nakashima, Akira Otaka & Nobutaka Fujii
Efficient Stereoselective Synthesis of Peptidomimetics Containing Hydroxyethylamine Dipeptide Isosteres Utilizing the Aza-Payne Rearrangement and O, N-Acyl Transfer Reactions.
J. Chem. Soc., Perkin Trans. 1, 2002(5), 577-580 (2002)
, Tadakazu Hori, Akira Otaka & Nobutaka Fujii
Development of Selective Antagonists against an HIV Second Receptor.
YAKUGAKU ZASSHI, 121(11), 781-792 (2001)- Nobutaka Fujii &
Peptide-lead CXCR4 Antagonists with High Anti-HIV Activity.
Curr. Opin. Invest. Drugs, 2(9), 1198-1202 (2001) - Shinya Oishi,
Stereoselective Synthesis of a Set of Two Functionalized (E)-Alkene Dipeptide Isosteres of L-Amino Acid-L-Glu and L-Amino acid-D-Glu.
J. Chem. Soc., Perkin Trans. 1, 2001(19), 2445-2451 (2001)
, Masaki Yamashita, Yoshihiko Odagaki, Nobuyuki Hamanaka, Akira Otaka & Nobutaka Fujii - Akira Otaka, Hideaki Watanabe, Akira Yukimasa, Shinya Oishi,
New Access to α-Substituted (Z)-Fluoroalkene Dipeptide Isosteres Utilizing Organocopper Reagents under ‘Reduction-oxidative Alkylation (R-OA)’ Conditions.
Tetrahedron Lett., 42(2), 5443-5446 (2001)
& Nobutaka Fujii
Synthesis and Evaluation of Bifunctional Anti-HIV Agents Based on Specific CXCR4 Antagonists-AZT Conjugation.
Bioorg. Med. Chem., 9(8), 2179-2187 (2001)
, Akane Omagari, Kenichi Hiramatsu, Taisei Kanamoto, Kazuyo Gotoh, Kenji Kanbara, Naoki Yamamoto, Hideki Nakashima, Akira Otaka & Nobutaka Fujii
Development of Specific CXCR4 Inhibitors Possessing High Selectivity Indexes as Well as Complete Stability in Serum Based on an Anti-HIV Peptide T140.
Bioorg. Med. Chem. Lett., 11(14), 1897-1902 (2001)
, Akane Omagari, Kenichi Hiramatsu, Kazuyo Gotoh, Taisei Kanamoto, Younong Xu, Eiichi Kodama, Masao Matsuoka, Toshio Hattori, Naoki Yamamoto, Hideki Nakashima, Akira Otaka & Nobutaka Fujii- Kenji Kanbara, Setsuko Sato, Jun-ichi Tanuma,
Biological and Genetic Characterization of a Human Immunodeficiency Virus Strain Resistant to CXCR4 Antagonist T134.
AIDS Res. Hum. Retroviruses, 17(7), 615-622 (2001)
, Kazuyo Gotoh, Manabu Yoshimori, Taisei Kanamoto, Motoo Kitano, Nobutaka Fujii & Hideki Nakashima - Kazuyo Gotoh, Manabu Yoshimori, Kenji Kanbara,
Increase of R5 HIV-1 Infection and CCR5 Expression in T cells Treated with High Concentrations of CXCR4 Antagonists and SDF-1.
J. Infect. Chemother., 7, 28-36 (2001)
, Taisei Kanamoto, Katsura Mochizuki, Nobutaka Fujii & Hideki Nakashima
Conformational Study of a Highly Specific CXCR4 Inhibitor, T140,Disclosing the Close Proximity of Its Intrinsic Pharmacophores Associated with Strong Anti-HIV Activity.
Bioorg. Med. Chem. Lett., 11(3), 359-362 (2001)
, Makiko Sugioka, Yoshihiko Odagaki, Akane Omagari, Yukiko Kan, Shinya Oishi, Hideki Nakashima, Naoki Yamamoto, Stephen C. Peiper, Nobuyuki Hamanaka, Akira Otaka & Nobutaka Fujii- Akira Otaka, Hideaki Watanabe, Etsuko Mitsuyama, Akira Yukimasa,
Synthesis of (Z)-Fluoroalkene Dipeptide Isosteres Utilizing Organocopper-Mediated Reduction of γ,γ-Difluoro-α,β-enoates.
Tetrahedron Lett., 42 (2), 285-287 (2001)
& Nobutaka Fujii
Pharmacophore Identification of a Specific CXCR4 Inhibitor, T140, Leads to Development of Effective Anti-HIV Agents with Very High Selectivity Indexes.
Bioorg. Med. Chem. Lett., 10(23), 2633-2637 (2000)
, Akane Omagari, Shinya Oishi, Taisei Kanamoto, Naoki Yamamoto, Stephen C. Peiper, Hideki Nakashima, Akira Otaka & Nobutaka Fujii- Keiko Udaka, Karl-Heinz Wiesmuller, Stefan Kienle, Gunther Jung,
An Automated Prediction of MHC Class 1-Binding Peptides Based on Positional Scanning with Peptide Libraties.
Immunogenetics, 51(10), 816-828 (2000)
, Hideo Yamagishi, Ko Okumura, Peter Walden, Taku Suto & Toshisuke Kawasaki - Akira Otaka, Etsuko Mitsuyama, Takayoshi Kinoshita,
Stereoselective Synthesis of CF2-Substituted Phosphothreonine Mimetics and Their Incorporation into Peptides Using Newly Developed Deprotection Procedure.
J. Org. Chem., 65, 4888-4899 (2000)
& Nobutaka Fujii
Conformationally Constrained Analogues of Diacylglycerol (DAG). 17. Contrast between sn-1 and sn-2 DAG Lactones in Binding to Protein Kinase C.
J. Med. Chem., 43, 3209-3217 (2000)
, Bruno Bienfait, Kassoum Nacro, Nancy E. Lewin, Peter M. Blumberg & Victor E. Marquez- Kengo Miyoshi, Akira Otaka, Midori Kaneko,
A New Practical Strategy for the Synthesis of Long-Chain Phosphopeptide.
Chem. Pharm. Bull., 48(8), 1230-1233 (2000)
& Nobutaka Fujii - Akira Otaka, Etsuko Mitsuyama, Hideaki Watanabe,
Development of New Methodology for the Synthesis of Functionalized -Fluorophosphonates and Its Practical Application to the Preparation of Phosphopeptide Mimetics.
Chem. Commun. , 2000, 1081-1082 (2000)
& Nobutaka Fujii - Kiyokazu Kakugawa, Keiko Udaka, Kosuke Nakashima, Kayo Inaba, Yoshihiro Oka, Haruo Sugiyama,
Efficient Induction of Peptide-Specific Cytotoxic T Lymphocytes by LPS-Activated Spleen Cells.
Microbiol. Immunol., 44(2), 123-133 (2000)
& Hideo Yamagishi - Tutomu Murakami, Tian-Yuan Zhang, Yoshio Koyanagi, Yuetsu Tanaka, Jin Kim, Yoichi Suzuki, Shigeru Minoguchi,
Inhibitory Mechanism of the CXCR4 Antagonist T22 against Human Immunodeficiency Virus Type 1 Infection.
J. Virol., 73(9), 7489-7496 (1999)
, Michinori Waki, Akiyoshi Matsumoto, Nobutaka Fujii, Hisatoshi Shida, James A. Hoxie, Stephen C. Peiper & Naoki Yamamoto
Regiospecific Ring-Opening Reactions of β-Aziridinyl α,β-Enoates with Acids: Application to the Stereoselective Synthesis of a Couple of Diastereoisomeric (E)-Alkene Dipeptide Isosteres from a Single β-Aziridinyl α,β-Enoate and to the Convenient Preparation of Amino Alcohols Bearing , -Unsaturated Ester Groups.
J. Chem. Soc., Perkin Trans. 1, 1999, 2983-2996 (1999)
, Masaki Yamashita, Yutaka Nakajima, Kyoko Sakano, Akira Otaka, Hiroaki Ohno, Toshiro Ibuka & Nobutaka Fujii- Younong Xu,
Marked Increase in Anti-HIV Activity, as Well as Inhibitory Activity against HIV Entry Mediated by CXCR4, Linked to Enhancement of the Binding Ability of Tachyplesin Analogs to CXCR4.
AIDS Res. Hum. Retroviruses, 15(5), 419-427 (1999)
, Rieko Arakaki, Hideki Nakashima, Xiaoyan Zhang, Nobutaka Fujii, Takashi Uchiyama & Toshio Hattori - Rieko Arakaki,
T134, a Small Molecule CXCR4 Inhibitor, Has No Cross Drug-Resistance with AMD3100, a CXCR4 Antagonist with a Different Structure.
J. Virol., 73(2), 1719-1723 (1999)
, Mariappan Premanathan, Kenji Kanbara, Sivasundaram Ramanan, Katsura Mochizuki, Masanori Baba, Nobutaka Fujii & Hideki Nakashima
A Low Molecular Weight Inhibitor against the Chemokine Receptor CXCR4: a Strong Anti-HIV Peptide T140.
Biochem. Biophys. Res. Commun., 253(3), 877-882 (1998)
, Younong Xu, Toshio Hattori, Xiaoyan Zhang, Rieko Arakaki, Kenji Kanbara, Akane Omagari, Akira Otaka, Toshiro Ibuka, Naoki Yamamoto, Hideki Nakashima & Nobutaka Fujii- Hiroaki Ohno, Kiyonori Ishii, Asami Honda,
A 2,3-cis-Selective Synthesis of Aziridines Bearing a Vinyl Group from Allyl Methyl Carbonates and Allyl Mesylates.
J. Chem. Soc., Perkin Trans. 1, 1998(22), 3703-3716 (1998)
, Nobutaka Fujii, Yoshiji Takemoto & Toshiro Ibuka - Hirohide Uenishi, Norimasa Iwanami, Hideo Yamagishi, Takako Nakatani, Toshisuke Kawasaki,
Induction of Crossreactivity in Endogenous Viral Peptide Non-reactive to FBL-3 Tumor-specific Helper T-Cell Clones.
Microbiol. Immunol., 42(7), 479-484 (1998)
, Nobutaka Fujii & Kagemasa Kuribayashi - Toshio Hattori, Haruko Komoda, Savita Pahwa, Masaki Tateyama, Xiaoyan Zhang, Younong Xu, Shigeru Oguma,
Decline of Anti-DP107 Antibody Associated with Clinical Progression.
AIDS, 12(12), 1557-1559 (1998)
, Nobutaka Fujii, Katuyuki Fukutake & Takashi Uchiyama - Hirohide Uenishi, Norimasa Iwanami, Kagemasa Kuribayashi,
Overlapping Epitopes of Friend Murine Leukemia Virus gag-Encoded Leader Sequence Recognized by Single Cytotoxic T-Lymphocyte Clones.
Immunology Lett., 62, 33-38 (1998)
, Nobutaka Fujii, Takako Nakatani, Toshisuke Kawasaki & Hideo Yamagishi
Pharmacophore Identification of a Chemokine Receptor (CXCR4) Antagonist, T22 ([Tyr5,12, Lys7]-Polyphemusin II), witch Specifically Blocks T Cell Line-Tropic HIV-1 Infection.
Bioorg. Med. Chem., 6(7), 1033-1041 (1998)
, Makoto Imai, Tsunehito Ishihara, Masao Masuda, Hanae Funakoshi, Hiromi Oyake, Tsutomu Murakami, Rieko Arakaki, Hideki Nakashima, Akira Otaka, Toshiro Ibuka, Michinori Waki, Akiyoshi Matsumoto, Naoki Yamamoto & Nobutaka Fujii
Downsizing of an HIV-Cell Fusion Inhibitor, T22 ([Tyr5,12, Lys7]-Polyphemusin II), with the Maintenance of Anti-HIV Activity and Solution Structure.
Bioorg. Med. Chem., 6(4), 473-479 (1998)
, Michinori Waki, Makoto Imai, Akira Otaka, Toshiro Ibuka, Koji Waki, Kenji Miyamoto, Akiyoshi Matsumoto, Tsutomu Murakami, Hideki Nakashima, Naoki Yamamoto & Nobutaka Fujii
Convenient One-pot Synthesis of Cystine-Containing Peptides Using the Trimethylsilyl Chloride-Dimethylsulfoxide/Trifluoroacetic Acid System and its Application to the Synthesis of Bifunctional Anti-HIV Compounds.
J. Chem. Soc., Perkin Trans. 1, 1998(3), 495-500 (1998)
, Tsunehito Ishihara, Hiromi Oyake, Makoto Imai, Akira Otaka, Toshiro Ibuka, Rieko Arakaki, Hideki Nakashima, Tsutomu Murakami, Michinori Waki, Akiyoshi Matsumoto, Naoki Yamamoto & Nobutaka Fujii
Effective Lowly Cytotoxic Analogs of an HIV-Cell Fuion Inhibitor, T22 ([Tyr5,12, Lys7]-polyphemusin II).
Bioorg. Med. Chem., 6(2), 231-238 (1998)
, Rieko Arakaki, Hanae Funakoshi, Makoto Imai, Akira Otaka, Toshiro Ibuka, Hideki Nakashima, Tsutomu Murakami, Michinori Waki, Akiyoshi Matsumoto, Naoki Yamamoto & Nobutaka Fujii
Unambiguous Synthesis of Stromal Cell-Derived Factor-1 by Regioselective Disulfide Bond Formation Using a DMSO-Aqueous HCl System.
Chem. Commun., 1998(1), 151-152 (1998)
, Fumihiro Matsumoto, Kyoko Sakano, Akira Otaka, Toshiro Ibuka & Nobutaka Fujii- Hiromu Habashita, Takeshi Kawasaki, Masako Akaji,
One-Pot Transformation of p-Toluenesulfonates of 2,3-Epoxy Alcohols into Allylic Alcohols.
Tetrahedron Lett., 38(48), 8307-8310 (1997)
, Tetsutaro Kimachi, Nobutaka Fujii & Toshiro Ibuka - Hiroshi Aoyama, Norio Mimura, Hiroaki Ohno, Kiyonori Ishii, Ayako Toda,
Regio- and Stereoselectivity in Reactions of 2,3-cis– and trans-3-Alkyl-2-vinylaziridines with Organocopper Reagents: Importance of 2,3-cis-Stereochemistry in Controlling Selectivity.
Tetrahedron Lett., 38(42), 7383-7386 (1997)
, Akira Otaka, Nobutaka Fujii & Toshiro Ibuka
Regiospecific Ring-Opening Reactions of Aziridines Bearing an α,β-Unsaturated Ester Group with Trifluoroacetic Acid or Methanesulfonic Acid: Application to the Stereoselective Synthesis of (E)-Alkene Dipeptide Isosteres.
Chem. Commun., 1997, 2327-2328 (1997)
, Masaki Yamashita, Hiroyuki Muramatsu, Hiroaki Ohno, Toshiro Ibuka, Akira Otaka & Nobutaka Fujii- Tsutomu Murakami, Toshihiro Nakajima, Yoshio Koyanagi, Kazunobu Tachibana, Nobutaka Fujii,
A Small Molecule CXCR4 Inhibitor that Blocks T Cell Line-tropic HIV-1 Infection.
J. Exp. Med., 186(8), 1389-1393 (1997)
, Nobuaki Yoshida, Michinori Waki, Akiyoshi Matsumoto, Osamu Yoshie, Tadamitsu Kishimoto, Naoki Yamamoto & Takashi Nagasawa - Hiroaki Ohno, Norio Mimura, Akira Otaka,
Palladium-Catalyzed Reductive Ring Opening with Formic Acid of Aziridines Bearing an α,β-Unsaturated Ester Group.
Tetrahedron, 53(38), 12933-12946 (1997)
, Nobutaka Fujii, Toshiro Ibuka, Isao Shimizu, Akiharu Satake & Yoshinori Yamamoto - Toshiro Ibuka, Norio Mimura, Hiroaki Ohno, Kazuo Nakai, Masako Akaji, Hiromu Habashita,
Palladium(o)-Catalyzed Isomerization Reactions of Aziridines Bearing an α,β-Unsaturated Ester Group: A Thermodynamic Preference for Chiral Alkyl (2E)-4,5-cis-4,5-Epimino-N-(alkyl- or arylsulfonyl) 2-Enoates over the Other Three Stereoisomers.
J. Org. Chem., 62(9), 2982-2991 (1997)
, Yoshihisa Miwa, Tooru Taga, Nobutaka Fujii & Yoshinori Yamamoto - Toshiro Ibuka, Norio Mimura, Hiroshi Aoyama, Masako Akaji, Hiroaki Ohno, Yoshihisa Miwa, Tooru Taga, Kazuo Nakai,
A Thermodynamic Preference of Chiral N-Methanesulfonyl and N-Arenesulfonyl 2,3-cis-3-Alkyl-2-vinylaziridines over Their 2,3-trans-Isomers: Useful Palladium(0)-Catalyzed Equilibration Reactions for the Synthesis of (E)-Alkene Dipeptide Isosters.
J. Org. Chem., 62(4), 999-1015 (1997)
, Nobutaka Fujii & Yoshinori Yamamoto
An Anti-HIV Peptide, T22, Forms a Highly Active Complex with Zn(II).
Biochem. Biophys. Res. Commun., 229, 648-652 (1996)
, Akira Otaka, Tsutomu Murakami, Toshiro Ibuka, Kyoko Sakano, Michinori Waki, Akiyoshi Matsumoto, Naoki Yamamoto & Nobutaka Fujii- Toshiro Ibuka, Kazuo Nakai, Masako Akaji,
An Aza-Payne Rearrangement-Epoxide Ring Opening Reaction of 2-Aziridinemethanols in a One-pot Manner: A Regio- and Stereoselective Synthetic Route to Diastereomerically Pure N-Protected 1,2-Amino Alcohols.
Tetrahedron, 52, 11739-11752 (1996)
, Nobutaka Fujii & Yoshinori Yamamoto
Analysis of the Interaction of an Anti-HIV Peptide, T22 ([Tyr5,12, Lys7]-Polyphemusin II), with Gp120 and CD4 by Surface Plasmon Resonance.
Biochim. Biophys. Acta, 1298, 37-44 (1996)
, Tsunehito Ishihara, Akira Otaka, Tsutomu Murakami, Toshiro Ibuka, Michinori Waki, Akiyoshi Matsumoto, Naoki Yamamoto & Nobutaka Fujii
A Convenient One-pot Synthesis of Cystine-Containing Peptides from Protected Peptidyl Resins Using the Trimethylsilyl Chloride-Dimethylsulfoxide-Trifluoroacetic Acid System.
J. Chem. Soc., Perkin Trans. 1 (Perkin Commun.), 1996, 1911-1912 (1996)
, Tsunehito Ishihara, Akira Otaka, Takaki Koide, Kengo Miyoshi, Toshiro Ibuka & Nobutaka Fujii- Michinori Waki, Koji Waki, Kenji Miyamoto, Akiyoshi Matsumoto,
Molecular Size of an Anti-HIV Peptide, T22, Can Be Reduced without Loss of the Activity.
Chem. Lett., 1996, 571-572 (1996)
, Nobutaka Fujii, Tsutomu Murakami, Hideki Nakashima & Naoki Yamamoto - Nobutaka Fujii, Hiromu Habashita, Masako Akaji, Kazuo Nakai, Toshiro Ibuka, Masahiro Fujiwara,
A Simple One-pot Transformation of p-Toluenesulfonates of 2,3-Epoxy Alcohols into Allylic Alcohols.
J. Chem. Soc., Perkin Trans. 1 (Perkin Commun.), 1996, 865-866 (1996)
& Yoshinori Yamamoto - Toshiro Ibuka, Masako Akaji, Norio Mimura, Hiromu Habashita, Kazuo Nakai,
A Thermodynamic Preference of Chiral cis-γ,δ-Epimino-(E)-α,β-Unsaturated Esters over Other Stereoisomers: Synthetically Useful Pd(0)-Catalyzed Equilibrated Reactions of Aziridines Bearing an α,β-Unsaturated Ester Groups.
Tetrahedron Lett., 37, 2849-2852 (1996)
, Nobutaka Fujii & Yoshinori Yamamoto - Norio Mimura, Toshiro Ibuka, Masako Akaji, Yoshihisa Miwa, Tooru Taga, Kazuo Nakai,
An Unusual Thermodynamic Preference of Chiral N-Arylsulfonyl cis-3-Alkyl-2-vinylaziridines over Theirtrans-Isomers: Palladium(0)-Catalyzed Equilibration Reaction.
J. Chem. Soc., Chem. Commun., 1996, 351-352 (1996)
, Nobutaka Fujii & Yoshinori Yamamoto
Interaction of an Anti-HIV Peptide, T22, with Gp120 and CD4.
Biochem. Biophys. Res. Commun., 219, 555-559 (1996)
, Akira Otaka, Tsutomu Murakami, Tsunehito Ishihara, Toshiro Ibuka, Michinori Waki, Akiyoshi Matsumoto, Naoki Yamamoto & Nobutaka Fujii- Tokukazu Kondo, Hirohide Uenishi, Takeyuki Shimizu, Toshiyasu Hirama, Michihiro Iwashiro, Kagemasa Kuribayashi,
A Signal Retroviral Gag Precursor Signal Peptide Recognized by FBL-3 Tumor-Specific Cytotoxic T Lymphocytes.
J. Virol., 69, 6735-6741 (1995)
, Nobutaka Fujii, Ryuichi Fujisawa, Masaaki Miyazawa & Hideo Yamagishi - Benjamin S. Weeks, Motoyoshi Nomizu, Akira Otaka, Christi A. Weston, Akiko Okusu,
The Synthetic [Tyr5,12, Lys7]-Polyphemusin II Peptide (T22) Binds to the CD4 Cell Surface Molecule.
Biochem. Biophys. Res. Commun., 215, 626-631 (1995)
, Naoki Yamamoto & Nobutaka Fujii - Kazuo Nakai, Toshiro Ibuka, Akira Otaka,
A One-pot Aza-Payne Rearrangement-Epoxide Ring Opening Reaction of 2-Aziridinemethanols: A Regio- and Stereoselective Synthetic Route to Diastereomerically Pure 1,2-Amino Alcohols.
Tetrahedron Lett., 36, 6247-6250 (1995)
, Nobutaka Fujii & Yoshinori Yamamoto - Akira Otaka, Kengo Miyoshi, Midori Kaneko,
Development of Efficient Two-Step Deprotection Methodology for Dimethyl-Protected Phosphoamino Acid-Containing Peptide Resins and Its Application to the Practical Synthesis of Phosphopeptides.
J. Org. Chem., 60, 3967-3974 (1995)
, Nobutaka Fujii, Motoyoshi Nomizu, Terrence R. Burke, Jr. & Peter P. Roller - Nobutaka Fujii, Kazuo Nakai,
SN2′ Ring Opening of Aziridines Bearing an α,β-Unsaturated Ester Group with Organocopper Reagents. A New Stereoselective Synthesis Route to (E)-Alkene Dipeptide Isosters.
J. Chem. Soc., Perkin Trans. 1, 1995, 1359-1371 (1995)
, Akira Otaka, Norio Mimura, Yoshihisa Miwa, Tooru Taga, Yoshinori Yamamoto & Toshiro Ibuka
Synthesis of Protegrin-Related Peptides and Their Antibacterial and Anti-Human Immunodeficiency Virus Activity.
Chem. Pharm. Bull., 43, 853-858 (1995)
, Tsutomu Murakami, Sankichi Horiuchi, Keiji Sugihara, Akira Otaka, Wataru Takada, Toshiro Ibuka, Michinori Waki, Naoki Yamamoto & Nobutaka Fujii- Toshiro Ibuka, Kazuo Nakai, Hiromu Habashita, Yuka Hotta, Akira Otaka,
Aza-Payne Rearrangement of Activated 2-Aziridinemethanols and 2,3-Epoxy Amines under Basic Conditions.
J. Org. Chem., 60, 2044-2058 (1995)
, Nobutaka Fujii, Norio Mimura, Yoshihisa Miwa, Tooru Taga, Yukiyasu Chounan & Yoshinori Yamamoto
Disulfide Bond-Forming Reaction using a Dimethyl Sulfoxide / Aqueous HCl System and Its Application to Regioselective Two Disulfide Bond Formation.
Int. J. Peptide Protein Res., 45, 312-319 (1995)
, Akira Otaka, Junko Nakamura, Kaori Okubo, Takaki Koide, Kyoko Ikeda, Toshiro Ibuka & Nobutaka Fujii- Akira Otaka, Kengo Miyoshi, Peter P. Roller, Terrence R. Burke, Jr.,
Practical Synthesis of Phosphopeptides using Dimethyl-protected Phosphoamino Acid Derivatives.
J. Chem. Soc., Chem. Commun., 1995, 387-389 (1995)
& Nobutaka Fujii - Akira Otaka, Kengo Miyoshi, Terrence R. Burke, Jr., Peter P. Roller, Hideki Kubota,
Synthesis and Application of N-Boc-L-2-amino-4-(diethylphosphono)-4, 4-difluorobutanoic acid for Solid-Phase Synthesis of Nonhydrolyzable Phosphoserine Peptide Analogs.
Tetrahedron Lett., 36, 927-930 (1995)
& Nobutaka Fujii
Solution-Phase Synthesis of an Anti-Human Immunodeficiency Virus Peptide, T22 ([Tyr5,12, Lys7]-Polyphemusin II), and the Modification of Trp by the p-Methoxybenzyl Group of Cys during Trimethylsilyl Trifluoromethanesulfonate Deprotection.
Chem. Pharm. Bull., 43, 12-18 (1995)
, Akira Otaka, Wataru Takada, Yoshihiro Terakawa, Hidenori Yoshizawa, Masao Masuda, Toshiro Ibuka, Tsutomu Murakami, Hideki Nakashima, Michinori Waki, Akiyoshi Matsumoto, Naoki Yamamoto & Nobutaka Fujii- Takeyuki Shimizu, Hirohide Uenishi, Yasufumi Teramura, Michihiro Iwashiro, Kagemasa Kuribayashi,
Fine Structure of a Virus-Encoded Helper T-Cell Epitope Expressed on FBL-3 Tumor Cells.
J. Virol., 68, 7704-7708 (1994)
, Nobutaka Fujii & Hideo Yamagishi
Structure-Activity Relationships of an Anti-HIV Peptide, T22.
Biochem. Biophys. Res. Commun., 205, 1729-1735 (1994)
, Tsutomu Murakami, Masao Masuda, Akira Otaka, Wataru Takada, Toshiro Ibuka, Hideki Nakashima, Michinori Waki, Akiyoshi Matsumoto, Naoki Yamamoto & Nobutaka Fujii- Akira Otaka,
Molecular Parameters for the Anti-Human Immunodeficiency Virus Activity of T22 ([Tyr5,12, Lys7]-Polyphemusin II).
Biol. Pharm. Bull., 17, 1669-1672 (1994)
, Yoshihiro Terakawa, Masao Masuda, Takaki Koide, Tsutomu Murakami, Hideki Nakashima, Katsumi Matsuzaki, Koichiro Miyajima, Toshiro Ibuka, Michinori Waki, Akiyoshi Matsumoto, Naoki Yamamoto & Nobutaka Fujii - Nobutaka Fujii, Kazuo Nakai, Hiromu Habashita, Yuka Hotta,
Synthesis of Optically Pure 2-Aziridinemethanols: Versatile Synthetic Building Blocks.
Chem. Pharm. Bull., 42, 2241-2250 (1994)
, Akira Otaka & Toshiro Ibuka - Toshiro Ibuka, Keisuke Suzuki, Hiromu Habashita, Akira Otaka,
(E)-Stereoselective Synthesis of Vinylglycines from (R)-Serine via Organocopper-BF3 and Related Reagents.
J. Chem. Soc., Chem. Commun., 1994, 2151-2152 (1994)
, Norio Mimura, Yoshihisa Miwa, Tooru Taga & Nobutaka Fujii - Benjamin S. Weeks, Motoyoshi Nomizu, Akira Otaka, Christi A. Weston, Akiko Okusu,
Lymphocytes and Promonocytes Attach to the Synthetic [Tyr5,12, Lys7]-Polyphemusin II Peptide.
Biochem. Biophys. Res. Commun., 202, 470-475 (1994)
, Akiyoshi Matsumoto, Naoki Yamamoto & Nobutaka Fujii
Disulfide Bond Formation in S-Acetamidomethyl Cysteine-Containing Peptides by the Combination of Silver Trifluoromethanesulfonate and Dimethylsulfoxide / Aqueous HCl.
Tetrahedron Lett., 34, 4931-4934 (1993)
, Akira Otaka, Junko Nakamura, Kaori Okubo, Takaki Koide, Kyoko Ikeda & Nobutaka Fujii
A Comparative Study of the Solution Structures of Tachyplesin I and a Novel Anti-HIV Synthetic Peptide, T22 ([Tyr5,12, Lys7]-Polyphemusin II), Determined by Nuclear Magnetic Resonance.
Biochim. Biophys. Acta, 1163, 209-216 (1993)
, Masataka Kuroda, Masao Masuda, Akira Otaka, Susumu Funakoshi, Hideki Nakashima, Naoki Yamamoto, Michinori Waki, Akiyoshi Matsumoto, Jean M. Lancelin, Daisuke Kohda, Shinichi Tate, Fuyuhiko Inagaki & Nobutaka Fujii
Antimicrobial Activity and Conformation of Tachyplesin I and Its Analogs.
Chem. Pharm. Bull., 41, 978-980 (1993)
, Rie Ikoma, Makoto Niwa, Susumu Funakoshi, Tsukasa Murakami & Nobutaka Fujii
Acceleration of Nα-Deprotection Rate by the Addition of m-Cresol to Diluted Methanesulfonic Acid and Its Application to the Z(OMe)-Based Solid-Phase Syntheses of Human Pancreastatin-29 and Magainin 1.
Chem. Pharm. Bull., 41, 954-957 (1993)
, Junko Nakamura, Katsuhiro Noguchi, Susumu Funakoshi & Nobutaka Fujii- Toshiro Ibuka, Tooru Taga, Hiromu Habashita, Kazuo Nakai,
Syn-SN2′ Pathway in the Reaction of Certain γ-(Mesyloxy)-α,β-Enoates with RCu(CN)MgX.BF3Reagents. Importance of MgX and Bulky R Group upon the Diastereoselectivity.
J. Org. Chem., 58, 1207-1214 (1993)
, Nobutaka Fujii, Yukiyasu Chounan, Hisao Nemoto & Yoshinori Yamamoto - Masao Masuda, Hideki Nakashima, Toshihiro Ueda, Hiroyasu Naba, Rie Ikoma, Akira Otaka, Yoshihiro Terakawa,
A Novel Anti-HIV Synthetic Peptide, T-22 ([Tyr5,12, Lys7]-Polyphemusin II).
Biochem. Biophys. Res. Commun., 189, 845-850 (1992)
, Toshiro Ibuka, Tsutomu Murakami, Yoshio Koyanagi, Michinori Waki, Akiyoshi Matsumoto, Naoki Yamamoto, Susumu Funakoshi & Nobutaka Fujii - Akihiro Funakoshi, Kyoko Miyasaka, Kenichi Kitani, Susumu Funakoshi,
Comparative Effects of Mammalian Pancreastatin on the Pancreatic Exocrine Secretion.
Japanese J. Pysiol., 39, 901-905 (1990)
, Nobutaka Fujii, Itsuro Nakano & Kazuhiko Tatemoto - Kyoko Miyasaka, Akihiro Funakoshi, Yohichi Yasunami, Rieko Nakamura, Kenichi Kitani,
Rat Pancreastatin Inhibits Both Pancreatic Exocrine and Endocrine Secretions in Rats.
Regulatory Peptides, 28, 189-198 (1990)
, Susumu Funakoshi & Nobutaka Fujii - Kyoko Miyasaka, Akihiro Funakoshi, Kenichi Kitani,
Inhibitory Effect of Pancreastatin on Pancreatic Exocrine Secretion. Pancreastatin Inhibits Central Vagel Nerve Stimulation.
Gastroenterology, 99, 1751-1756 (1990)
, Susumu Funakoshi & Nobutaka Fujii
Isolation and Characterization of a Tumor-Derived Human Protein Related to Chromogranin A and Its in Vitro Conversion to Human Pancreastatin-48.
Eur. J. Biochem., 191, 33-39 (1990)
, Mitsuhiro Ohta, Kumi Yoshizawa, Yoshiyuki Ono, Akihiro Funakoshi, Kyoko Miyasaka, Kayoko Tateishi, Atsuo Jimi, Haruaki Yajima, Nobutaka Fujii & Susumu Funakoshi- Kyoko Miyasaka, Akihiro Funakoshi, Kenichi Kitani,
The Importance of the C-Terminal Amide Structure of Rat Pancreastatin to Inhibit Pancreatic Exocrine Secretion.
FEBS Lett., 263, 279-280 (1990)
, Nobutaka Fujii & Susumu Funakoshi - Kayoko Tateishi, Akihiro Funakoshi, Hideyuki Wakasugi, Haruo Iguchi, Hirotsugu Shinozaki, Muneaki Abe, Susumu Funakoshi,
Plasma Pancreastatin-Like Immunoreactivity in Various Diseases.
J. Clin. Endocrin. and Metabo., 69, 1305-1308 (1989)
, Haruaki Yajima & Yuji Matsuoka - Susumu Funakoshi,
Isolation and Characterization of a Tumor-Derived Human Pancreastatin-Related Protein.
Biochem. Biophys. Res. Commun., 164, 141-148 (1989)
, Mitsuhiro Ohta, Kumi Yoshizawa, Akihiro Funakoshi, Kyoko Miyasaka, Kayoko Tateishi, Kazuhiko Tatemoto, Itsuro Nakano, Haruaki Yajima & Nobutaka Fujii - Akihiro Funakoshi, Atsuo Jimi, Yohichi Yasunami, Kayoko Tateishi, Susumu Funakoshi,
Bioactivity of Human Pancreastatin and Its Localization of Pancreas.
Biochem. Biophys. Res. Commun., 159, 913-918 (1989)
& Haruaki Yajima - Akihiro Funakoshi, Kyoko Miyasaka, Kenichi Kitani,
Bioactivity of Synthetic C-Terminal Fragment of Rat Pancreastatin on Endocrine Pancreas.
Biochem. Biophys. Res. Commun., 158, 844-849 (1989)
, Susumu Funakoshi & Haruaki Yajima - Kayoko Tateishi, Akihiro Funakoshi, Atsuo Jimi, Susumu Funakoshi,
High Plasma Pancreastatinlike Immunoreactivity in a Patient with Malignant Insulinoma.
Gastroenterology, 97, 1313-1318 (1989)
, Haruaki Yajima & Yuji Matsuoka - Nobutaka Fujii, Akira Otaka, Toshihiro Watanabe, Akira Okamachi,
Silver Trifluoromethanesulphonate as an S-Deprotecting Reagent for the Synthesis of Cystine Peptides.
J. Chem. Soc., Chem. Commun., 1989, 283-284 (1989)
, Haruaki Yajima, Yoshimasa Inagaki, Motoyoshi Nomizu & Katsuhiko Asano - Akihiro Funakoshi, Kyoko Miyasaka, Rieko Nakamura, Kenichi Kitani, Susumu Funakoshi,
Bioactivity of Synthetic Human Pancreastatin on Exocrine Pancreas.
Biochem. Biophys. Res. Commun., 156, 1237-1242 (1988)
, Nobutaka Fujii & Haruaki Yajima - Susumu Funakoshi,
Combination of a New Amide-precursor Reagent and Trimethylsilyl Bromide Deprotection for the Fmoc-based Solid Phase Synthesis of Human Pancreastatin and One of its Fragment.
J. Chem. Soc., Chem. Commun., 1988, 1588-1590 (1988)
, Nobutaka Fujii, Kumi Yoshizawa, Haruaki Yajima, Kyoko Miyasaka, Akihiro Funakoshi, Mitsuhiro Ohta, Yoshimasa Inagaki & Louis A. Carpino