論文・出版物等

2024 | 2023 | 2022 | 2021 | 2020 | 2019 | 2018 | 2017 | 2016 | 2015 | 2014 | 2013 | 2012 | 2011 | 2010 | 2009 | 2008 |

2024

Discovery of novel binders to sterol regulatory element-binding protein-1 by high-throughput screening
Takashi Maruyama, Yu Takahashi, Kahori Hiro, Kohji Murase, Hirotatsu Kojima, Takayoshi Okabe, Yoshio Yamauchi, Ryuichiro Sato, ACS Med. Chem. Lett. in press.
Reduction of amyloid-β production without inhibiting secretase activity by MS-275
Yachiyo Mitsuishi, Masaki Nakano, Hirotatsu Kojima, Takayoshi Okabe, Masaki Nishimura, ACS Chem. Neurosci. 15, 1234–1241 (2024) doi: 10.1021/acschemneuro.3c00848.
Chemical inhibition of phosphatidylcholine biogenesis reveals its role in mitochondrial division
Hiroya Shiino, Shinya Tashiro, Michiko Hashimoto, Yuki Sakata, Takamitsu Hosoya, Toshiya Endo, Hirotatsu Kojima, Yasushi Tamura, iScience 27, 109189 (2024) doi: 10.1016/j.isci.2024.109189.
東京大学創薬機構のアカデミア創薬研究支援と将来に向けた取り組み
金光佳世子, 小島宏建, 実験医学増刊「あなたのラボから薬を生み出す　アカデミア創薬の実践」42, 162–169 (2024).
ヒット探索の強化に向けたDNA-encoded libraryプラットフォームの構築―産学共創で日本の創薬研究を加速する
佐々木潤子, 安田公助, 実験医学増刊「あなたのラボから薬を生み出す　アカデミア創薬の実践」42, 330–336 (2024).
A newly identified compound activating UCP1 inhibits obesity and its-related metabolic disorders
Ken Onodera, Yutaka Hasegawa, Nozomi Yokota, Shukuko Tamura, Hirofumi Kinno, Iwao Takahashi, Hiraku Chiba, Hirotatsu Kojima, Hideki Katagiri, Koji Nata, Yasushi Ishigaki, Obesity 32, 324338 (2024) doi: 10.1002/oby.23948.
AKT2 inhibition accelerates the acquisition of phagocytic ability in iPSCs-derived neutrophils
Toshiya Hino, Fumio Nakahara, Masashi Miyauchi, Yusuke Ito, Yosuke Masamoto, Ken Morita, Yuki Kagoya, Hirotatsu Kojima, Mineo Kurokawa, Exp Hematol 130, 104137 (2024) doi: 10.1016/j.exphem.2023.104137.

2023

2-thiouridine is a broad-spectrum antiviral nucleoside analogue against positive-strand RNA viruses
Kentaro Uemura, Haruaki Nobori, Akihiko Sato, Shinsuke Toba, Shinji Kusakabe, Michihito Sasaki, Koshiro Tabata, Keita Matsuno, Naoyoshi Maeda, Shiori Ito, Mayu Tanaka, Yuki Anraku, Shunsuke Kita, Mayumi Ishii, Kayoko Kanamitsu, Yasuko Orba, Yoshiharu Matsuura, William W Hall, Hirofumi Sawa, Hiroshi Kida, Akira Matsuda, Katsumi Maenaka, Proc. Natl. Acad. Sci. USA 120, e2304139120 (2023) doi: 10.1073/pnas.2304139120.
Discovery of a cystathionine γ-lyase (CSE) selective inhibitor targeting active-site pyridoxal 5′-phosphate (PLP) via Schiff base formation
Honami Echizen, Kenjiro Hanaoka, Kazuhito Shimamoto, Ryota Hibi, Sachiko Toma-Fukai, Hisashi Ohno, Eita Sasaki, Toru Komatsu, Tasuku Ueno, Yukihiro Tsuchiya, Yasuo Watanabe, Takao Otsuka, Hiroaki Saito, Satoru Nagatoishi, Kouhei Tsumoto, Hirotatsu Kojima, Takayoshi Okabe, Toshiyuki Shimizu, Yasuteru Urano, Sci. Rep. 13, 16456 (2023) doi: 10.1038/s41598-023-43536-6.
Restoration of cardiac myosin light chain kinase ameliorates systolic dysfunction by reducing super-relaxed myosin
Tatsuro Hitsumoto, Osamu Tsukamoto, Ken Matsuoka, Junjun Li, Li Liu, Yuki Kuramoto, Noboru Fujino, Shohei Yoshida, Shuichiro Higo, Shou Ogawa, Hidetaka Kioka, Hisakazu Kato, Hideyuki Hakui, Yuki Saito, Chisato Okamoto, Hijiri Inoue, Hyejin Jo, Kyoko Ueda, Takatsugu Segawa, Shunsuke Nishimura, Yoshihiro Asano, Hiroshi Asanuma, Akiyoshi Tani, Riyo Imamura, Shinsuke Komagawa, Toshio Kanai, Masayuki Takamura, Yasushi Sakata, Masafumi Kitakaze, Jun-ichi Haruta, and Seiji Takashima, Circulation 147, 1902–1918 (2023) doi: 10.1161/CIRCULATIONAHA.122.062885.
Development of pathway-oriented screening to identify compounds to control 2-methylglyoxal metabolism in tumor cells
Kouichi Yanagi, Toru Komatsu, Yuuta Fujikawa, Hirotatsu Kojima, Takayoshi Okabe, Tetsuo Nagano, Tasuku Ueno, Kenjiro Hanaoka and Yasuteru Urano, Commun. Chem. 6, 68 (2023) doi: 10.1038/s42004-023-00864-y.
Drug cytotoxicity screening using human intestinal organoids propagated with extensive cost-reduction strategies
Yu Takahashi, Yu Inoue, Shintaro Sato, Takayoshi Okabe, Hirotatsu Kojima, Hiroshi Kiyono, Makoto Shimizu, Yoshio Yamauchi, Ryuichiro Sato, Sci. Rep. 13, 5407 (2023) doi: 10.1038/s41598-023-32438-2.

2022

Roles of peptidyl prolyl isomerase Pin1 in viral propagation [Mini Review]
Machi Kanna, Yusuke Nakatsu, Takeshi Yamamotoya, Jeffrey Encinas, Hisanaka Ito, Takayoshi Okabe, Tomoichiro Asano, Takemasa Sakaguchi, Front. Cell Dev. Biol. 10, 1005325 (2022) doi: 10.3389/fcell.2022.1005325.
Chlorinated Naringenin Analogues as Potential Inhibitors of Transthyretin Amyloidogenesis
Mineyuki Mizuguchi, Yusuke Nakagawa, Kishin Inui, Wakana Katayama, Yurika Sawai, Ayaka Shimane, Ryota Kitakami, Takuya Okada, Yuko Nabeshima, Takeshi Yokoyama, Kayoko Kanamitsu, Shinsaku Nakagawa, Naoki Toyooka, J. Med. Chem. 65, 16218–16233 (2022) doi: 10.1021/acs.jmedchem.2c00511.
Crystal structures of the ligand-binding domain of human peroxisome proliferator-activated receptor δ in complexes with phenylpropanoic acid derivatives and a pyridine carboxylic acid derivative
Kenta Nishitani, Koji Hayakawa, Masayuki Minatomoto, Keisuke Tanaka, Hidehiko Ogawa, Hirotatsu Kojima, Satoshi Tanaka, Biochem. Biophys. Res. Commun. 636, 205−212 (2022) doi: 10.1016/j.bbrc.2022.10.085
Development of p62-Keap1 protein-protein interaction inhibitors as doxorubicin-sensitizers against non-small cell lung cancer
Daisuke Yasuda, Ippei Yoshida, Riyo Imamura, Daiki Katagishi, Kyoko Takahashi, Hirotatsu Kojima, Takayoshi Okabe, Yoshinobu Ichimura, Masaaki Komatsu, Tadahiko Mashino, Tomoyuki Ohe, Results Chem. 4, 100609 (2022) doi: 10.1016/j.rechem.2022.100609.
Dephospho coenzyme A kinase is an exploitable drug target against Plasmodium falciparum: identification of selective inhibitors by high-throughput screening of large chemical compound library
Arif Nurkanto, Riyo Imamura, Yulia Rahmawati, Erwahyuni Prabandari, Danang Wayulo, Takeshi Annoura, Kazuki Yamamoto, Masakazu Sekijima, Yuki Nishimura, Takayoshi Okabe, Tomoo Shiba, Shibata Norio, Hirotatsu Kojima, James Duffy, Tomoyoshi Nozaki, Antimicrob. Agents Chemother. 66, e0042022 (2022) doi: 10.1128/aac.00420-22.
Conversion of a PROTAC Mutant Huntingtin Degrader into Small-Molecule Hydrophobic Tags Focusing on Drug-like Properties
Keigo Hirai, Hiroko Yamashita, Shusuke Tomoshige, Yugo Mishima, Tatsuya Niwa, Kenji Ohgane, Mayumi Ishii, Kayoko Kanamitsu, Yui Ikemi, Shinsaku Nakagawa, Hideki Taguchi, Shinichi Sato, Yuichi Hashimoto, Minoru Ishikawa, ACS Med. Chem. Lett. 13, 396–402 (2022) doi: 10.1021/acsmedchemlett.1c00500.
Crystal structures of the ligand-binding domain of human peroxisome proliferator-activated receptor δ in complexes with phenylpropanoic acid derivatives and a pyridine carboxylic acid derivative
Takuji Oyama, Kazuki Takiguchi, Hiroyuki Miyachi, Acta Crystallogr. Sect. F, Struct. Biol. Commun. 78, 81–87 (2022) doi: 10.1107/S2053230X22000449.
Arylalkynyl amide-type peroxisome proliferator-activated receptor γ (PPARγ)-selective antagonists covalently bind to the PPARγ ligand binding domain with a unique binding mode
Mami Yoshizawa, Tomomi Aoyama, Toshimasa Itoh, Hiroyuki Miyachi, Bioorg. Med. Chem. Lett. 64, 128676 (2022) doi: 10.1016/j.bmcl.2022.128676.
実験医学別冊創薬研究のためのスクリーニング学実践テキスト -アッセイ系の選択・構築から、ヒット・リード化合物の同定、自動化まで-
今村理世, 長谷川司, 岡部隆義他著, 新井好史, 岡部隆義編, 羊土社 (2022).
Small-molecule-induced activation of cellular respiration inhibits biofilm formation and triggers metabolic remodeling in Staphylococcus aureus
Ken-ichi Okuda, Satomi Yamada-Ueno, Yutaka Yoshii, Tetsuo Nagano, Takayoshi Okabe, Hirotatsu Kojima, Yoshimitsu Mizunoe, Yuki Kinjo, mBio 13, e00845-22 (2022) doi: 10.1128/mbio.00845-22.
Ligand recognition by the lipid transfer domain of human OSBP is important for enterovirus replication
Jun Kobayashi, Minetaro Arita, Shota Sakai, Hirotatsu Kojima, Miki Senda, Toshiya Senda, Kentaro Hanada, Ryuichi Kato, ACS Infect. Dis. 8, 1161–1170 (2022) doi: 10.1021/acsinfecdis.2c00108.
Organoid-derived intestinal epithelial cells are a suitable model for preclinical toxicology and ADME studies
Yu Takahashi, Makoto Noguchi, Yu Inoue, Shintaro Sato, Makoto Shimizu, Hirotatsu Kojima, Takayoshi Okabe, Hiroshi Kiyono, Yoshio Yamauchi, Ryuichiro Sato, iScinece 25, 104542 (2022) doi: 10.1016/j.isci.2022.104542.
Application of acoustic ejection MS system to high-throughput screening for SARS-CoV-2 3CL protease inhibitors
Tsukasa Hasegawa, Riyo M. Imamura, Tateki Suzuki, Takao Hashiguchi, Takao Nomura, Satoko Otsuguro, Katsumi Maenaka, Michihito Sasaki, Yasuko Orba, Hirofumi Sawa, Akihiko Sato, Takayoshi Okabe, Tetsuo Nagano, Hirotatsu Kojima, Chem. Pharm. Bull. 70, 199–201 (2022) doi: 10.1248/cpb.c21-01003.
Molecular action of larvicidal flavonoids on ecdysteroidogenic glutathione S-transferase Noppera-bo in Aedes aegypti
Kazue Inaba, Kana Ebihara, Miki Senda, Ryunosuke Yoshino, Chisako Sakuma, Kotaro Koiwai, Daisuke Takaya, Chiduru Watanabe, Yusuke Kawashima, Kaori Fukuzawa, Riyo Imamura, Hirotatsu Kojima, Takayoshi Okabe, Nozomi Uemura, Shinji Kasai, Hirotaka Kanuka, Takashi Nishimura, Kodai Watanabe, Hideshi Inoue, Yuuta Fujikawa, Teruki Honma, Takatsugu Hirokawa, Toshiya Senda, Ryusuke Niwa, BMC Biol. 20, 43 (2022) doi: 10.1186/s12915-022-01233-2.
次世代医薬とバイオ医療
安田公助他著, 長野哲雄, 川西徹編　東京化学同人 (2022).

2021

Prolyl isomerase Pin1 plays an essential role in SARS-CoV-2 proliferation, indicating its possibility as a novel therapeutic target
Takeshi Yamamotoya, Yusuke Nakatsu, Machi Kanna, Shun Hasei, Yukino Ohata, Jeffrey Encinas, Hisanaka Ito, Takayoshi Okabe, Tomoichiro Asano, Takemasa Sakaguchi, Sci. Rep. 11(1), 18581 (2021) doi: 10.1038/s41598-021-97972-3.J.
Synthesis and Evaluation of Quinone Derivatives for Activity against Trypanosome cruzi
Yutaka Suto, Tatiana Ascencio, Tomoya Nobuta, Noriyuki Yamagiwa, Yoko Onizuka, Mayumi Ishii, Kayoko Kanemitsu, Junko Nakajima-Shimada, Chem. Pharm. Bull. 69, 1195–1199 (2021) doi: 10.1248/cpb.c21-00732.
Photoelectric Dye, NK-5962, as a Potential Drug for Preventing Retinal Neurons from Apoptosis: Pharmacokinetic Studies Based on Review of the Evidence
Matsuo T, Liu S, Uchida T, Onoue S, Nakagawa S, Ishii M, Kanamitsu K., Life (Basel) 11, 591 (2021) doi: 10.3390/life11060591.
Inhibitory activities of anthraquinone and xanthone derivatives against transthyretin amyloidogenesis
Kitakami R, Inui K, Nakagawa Y, Sawai Y, Katayama W, Yokoyama T, Okada T, Kanamitsu K, Nakagawa S, Toyooka N, Mizuguchi M., Bioorg. Med. Chem. 44, 116292 (2021) doi: 10.1016/j.bmc.2021.116292.
Crystal Structures of the Human Peroxisome Proliferator-Activated Receptor (PPAR)α Ligand-Binding Domain in Complexes with a Series of Phenylpropanoic Acid Derivatives Generated by a Ligand-Exchange Soaking Method
Takuji Oyama, Shotaro Kamata, Isao Ishii, Hiroyuki Miyachi, Bio. Pharm. Bull. 44, 1202–1209 (2021) doi: 10.1248/bpb.b21-00220.
Structural Biology-Based Exploration of Subtype-Selective Agonists for Peroxisome Proliferator-Activated Receptors
Hiroyuki Miyachi, Int. J. Mol. Sci. 22, 9223 (2021) doi: 10.3390/ijms22179223.
Pathological Role of Pin1 in the Development of DSS-Induced Colitis
Yasuka Matsunaga, Shun Hasei, Takeshi Yamamotoya, Hiroaki Honda, Akifumi Kushiyama, Hideyuki Sakoda, Midori Fujishiro, Hiraku Ono, Hisanaka Ito, Takayoshi Okabe, Tomoichiro Asano, Yusuke Nakatsu, Cells, 10(5), 1230 (2021) doi: 10.3390/cells10051230J.
Establishment of live-cell-based coupled assay system for identification of compounds to modulate metabolic activities of cells
Kouichi Yanagi, Toru Komatsu, Shusuke Ogihara, Takayoshi Okabe, Hirotatsu Kojima, Tetsuo Nagano, Tasuku Ueno, Kenjiro Hanaoka, Yasuteru Urano, Cell Rep. 36, 109311 (2021) doi: 10.1016/j.celrep.2021.109311.
Supporting drug discovery research in Japan by Drug Discovery Initiative at the University of Tokyo
Hirotatsu Kojima, Burger’s Medicinal Chemistry, Drug Discovery and Development 8th Ed., Wiley, Abraham, D.J., Myers M. ed. 3, 179-187 (2021).
Non-steroidal inhibitors of Drosophila melanogaster steroidogenic glutathione S-transferase Noppera-bo
Kotaro Koiwai, Kana Morohashi, Kazue Inaba, Kana Ebihara, Hirotatsu Kojima, Takayoshi Okabe, Ryunosuke Yoshino, Takatsugu Hirokawa, Taiki Nampo, Yuuta Fujikawa, Hideshi Inoue, Fumiaki Yumoto, Toshiya Senda, Ryusuke Niwa, J. Pestic. Sci. 46, 75-87 (2021) doi: 10.1584/jpestics.D20-072.
Identification of novel juvenile-hormone signaling activators via high-throughput screening with a chemical library
Takumi Kayukawa, Kenjiro Furuta, Kiyoaki Yonesu, Takayoshi Okabe, J. Pestic. Sci. 46, 53-59 (2021) doi: 10.1584/jpestics.D20-070.
アカデミア創薬Hit to Lead支援の最前線：東京大学創薬機構構造展開ユニットのあゆみ
宮地弘幸, 安田公助, 金光佳世子, 榑林陽一, MEDCHEM NEWS 31(1),13-16 (2021).
Structure, solubility, and permeability relationships in a diverse middle molecule library
Hiroyuki Miyachi, Kayoko Kanamitsu, Mayumi Ishii, Eri, Watanabe, Akira Katsuyama, Satoko Otsuguro, Fumika Yakushiji, Mizuki Watanabe, Kouhei Matsui, Yukina Sato, Satoshi Shuto, Takashi Tadokoro, Shunsuke Kita, Takanori Matsumaru, Akira Matsuda, Tomoyasu Hirose, Masato Iwatsuki, Yasuteru Shigeta, Tetsuo Nagano, Hirotatsu Kojima, Satoshi Ichikawa, Toshiaki Sunazuka, Katsumi Maenaka, Bioorg. Med. Chem. Lett. 37, 127847 (2021) doi: 10.1016/j.bmcl.2021.127847.
Identification of novel compounds that inhibit SnRK2 kinase activity by high-throughput screening
Shoko Matsuoka, Karin Sato, Riyo Maruki-Imamura, Yoshiteru Noutoshi, Takayoshi Okabe, Hirotatsu Kojima, Taishi Umezawa, Biochem. Biophys. Res. Commun. 537, 57-63 (2021) doi: 10.1016/j.bbrc.2020.12.046.
Discovery of Carbono(di)thioates as Indoleamine 2,3-Dioxygenase 1 Inhibitors
Miyuki Kumazawa, Manabu Tejima, Miwa Fukuda, Shota Takeda, Kenji Suzuki, Yukiko Mizumoto, Kakeru Sato, Minoru Waki, Hiroyuki Miyachi, Akira Asai, Osamu Takikawa, Tomoko Hashimoto, Osamu Ohno, Kenji Matsuno, ACS Med. Chem. Lett. 12, 211-216 (2021) doi: 10.1021/acsmedchemlett.0c00527.

2020

Inhibitors of the protein-protein interaction between phosphorylated p62 and Keap1 attenuate chemoresistance in a human hepatocellular carcinoma cell line
Daisuke Yasuda, Tomoyuki Ohe, Kyoko Takahashi, Riyo Imamura, Hirotatsu Kojima, Takayoshi Okabe, Yoshinobu Ichimura, Masaaki Komatsu, Masayuki Yamamoto, Tetsuo Nagano and Tadahiko Mashino, Free Radical Research, 54, 859–871 (2020) doi: 10.1080/10715762.2020.1732955.
Identification of a juvenile-hormone signaling inhibitor via high-throughput screening of a chemical library
Takumi Kayukawa, Kenjiro Furuta, Keisuke Nagamine, Tetsuro Shinoda, Kiyoaki Yonesu, Takayoshi Okabe, Sci. Rep. 10, 18413 (2020) doi: 10.1038/s41598-020-75386-x.
An integrated approach to unravel a crucial structural property required for the function of the insect steroidogenic Halloween protein Noppera-bo
Kotaro Koiwai, Kazue Inaba, Kana Morohashi, Sora Enya, Reina Arai, Hirotatsu Kojima, Takayoshi Okabe, Yuuta Fujikawa, Hideshi Inoue, Ryunosuke Yoshino, Takatsugu Hirokawa, Koichiro Kato, Kaori Fukuzawa, Yuko Shimada-Niwa, Akira Nakamura, Fumiaki Yumoto, Toshiya Senda, Ryusuke Niwa, J. Biol. Chem. 295, 7154-7167 (2020) doi: 10.1074/jbc.RA119.011463.
Identification of potent in vivo autotaxin inhibitors that bind to both hydrophobic pocket and channel in the catalytic domain
Mitsuyasu Kawaguchi, Takayoshi Okabe, Shinichi Okudaira, Kotaro Hama, Kuniyuki Kano, Hiroshi Nishimasu, Hidehiko Nakagawa, Ryuichiro Ishitani, Hirotatsu Kojima, Osamu Nureki, Junken Aoki, Tetsuo Nagano, J. Med. Chem. 63, 3188-3204 (2020) doi: 10.1021/acs.jmedchem.9b01967.
Targeting FROUNT with disulfiram suppresses macrophage accumulation and its tumor-promoting properties
Yuya Terashima, Etsuko Toda, Meiji Itakura, Mikiya Otsuji, Sosuke Yoshinaga, Kazuhiro Okumura, Francis H. W. Shand, Yoshihiro Komohara, Mitsuhiro Takeda, Kana Kokubo, Ming-Chen Chen, Sana Yokoi, Hirofumi Rokutan, Yutaka Kofuku, Koji Ohnishi, Miki Ohira, Toshihiko Iizasa, Hirofumi Nakano, Takayoshi Okabe, Hirotatsu Kojima, Akira Shimizu, Shiro Kanegasaki, Ming-Rong Zhang, Ichio Shimada, Hiroki Nagase, Hiroaki Terasawa, and Kouji Matsushima, Nat. Commun. 11, 609 (2020).
Metabolic-pathway-oriented screening targeting S-adenosyl-l-methionine reveals the epigenetic remodeling activities of naturally occurring catechols
Shusuke Ogihara, Toru Komatsu, Yukihiro Itoh, Yuka Miyake, Takayoshi Suzuki, Kouichi Yanagi, Yusuke Kimura, Tasuku Ueno, Kenjiro Hanaoka, Hirotatsu Kojima, Takayoshi Okabe, Tetsuo Nagano, and Yasuteru Urano, J. Am. Chem. Soc. 142, 21–26 (2020) doi: 10.1021/jacs.9b08698.
Analysis of binding affinity and docking of novel fatty acid-binding protein (FABP) ligands
Yasuharu Shinoda, Yifei Wang, Tetsunori Yamamoto, Hiroyuki Miyachi, Kohji Fukunaga, J. Pharmacol. Sci. 143, 264–271 (2020) doi: 10.1016/j.jphs.2020.05.005.
Structural Basis for PPARα Activation by 1H-pyrazolo-[3,4-b]pyridine Derivatives
Takuya Yoshida, Hiroya Oki, Michihiro Doi, Syohei Fukuda, Tomohiro Yuzuriha, Ryotaro Tabata, Kenji Ishimoto, Kazuki Kawahara, Tadayasu Ohkubo, Hiroyuki Miyachi, Takefumi Doi, Keisuke Tachibana, Sci. Rep. 10, 7623 (2020) doi: 10.1038/s41598-020-64527-x.
Novel fatty acid-binding protein 3 ligand inhibits dopaminergic neuronal death and improves motor and cognitive impairments in Parkinson’s disease model mice
Hidaka Haga, Ryo Yamada, Hisanao Izumi, Yasuharu Shinoda, Ichiro Kawahata, Hiroyuki Miyachi, Kohji Fukunaga, Pharmacol. Biochem. Behav. 191, 172891 (2020) doi: 10.1016/j.pbb.2020.172891.
低分子医薬品今昔
宮地弘幸, 化学と教育 68(7), 282–285 (2020) doi: 10.20665/kakyoshi.68.7_282.
バイオ医薬　基礎から開発まで
石井明子, 川西徹, 長野哲雄編　東京化学同人 (2020).

2019

Cell-based HTS identifies a chemical chaperone for preventing ER protein aggregation and proteotoxicity
Keisuke Kitakaze, Shusuke Taniuchi, Eri Kawano, Yoshimasa Hamada, Masato Miyake, Miho Oyadomari, Hirotatsu Kojima, Hidetaka Kosako, Tomoko Kuribara, Suguru Yoshida, Takamitsu Hosoya, Seiichi Oyadomari, eLife 8, e43302 (2019) doi: 10.7554/eLife.43302
Development of a Novel Intraocular-Pressure-Lowering Therapy Targeting ATX
Norimichi Nagano, Megumi Honjo, Mitsuyasu Kawaguchi, Hiroshi Nishimasu, Osamu Nureki, Kuniyuki Kano, Junken Aoki, Toru Komatsu, Takayoshi Okabe, Hirotatsu Kojima, Tetsuo Nagano and Makoto Aihara, Biol. Pharm. Bull. 42, 1926-1935 (2019).
Oxytocin/vasopressin-like peptide inotocin regulates cuticular hydrocarbon synthesis and water balancing in ants
Akiko Koto, Naoto Motoyama, Hiroki Tahara, Sean McGregor, Minoru Moriyama, Takayoshi Okabe, Masayuki Miura, and Laurent Keller, PNAS 116, 5597-5606 (2019) DOI: 10.1073/pnas.1817788116.
Stability of the ABCD1 Protein with a Missense Mutation: A Novel Approach to Finding Therapeutic Compounds for X-Linked Adrenoleukodystrophy
Masashi Morita, Shun Matsumoto, Airi Sato, Kengo Inoue, Dzmitry G. Kostsin, Kozue Yamazaki, Kosuke Kawaguchi, Nobuyuki Shimozawa, Stephan Kemp, Ronald J. Wanders, Hirotatsu Kojima, Takayoshi Okabe, Tsuneo Imanaka, JIMD Rep. 44, 23-31 (2019).
Inexpensive High-Throughput Screening of Kinase Inhibitors Using One-step Enzyme-Coupled Fluorescence Assay for ADP Detection
Riyo Maruki Imamura, Kazuo Kumagai, Hirofumi Nakano, Takayoshi Okabe, Tetsuo Nagano and Hirotatsu Kojima, SLAS Discovery 24, 284-294 (2019).
Structural development of 1H-pyrazolo-[3,4-b]pyridine-4-carboxylic acid derivatives as human peroxisome proliferator-activated receptor alpha (PPARα)-selective agonists
Hiroyuki Miyachi, Tomohiro Yuzuriha, Ryotaro Tabata, Syohei Fukuda, Kazuto Nunomura, Bangzhong Lin, Tadayuki Kobayashi, Kenji Ishimoto, Takefumi Doi, Keisuke Tachibana, Bioorg. Med. Chem. Lett. 29, 2124-2128 (2019). doi: 10.1016/j.bmcl.2019.06.062
Translational science: Key features, issues and future perspectives
Yoichi Kurebayashi, Translat. Regulat. Sci. 1, 1-3 (2019). doi: 10.33611/trs.1_1
Inhibition of MPTP-induced α-synuclein oligomerization by fatty acid-binding protein 3 ligand in MPTP-treated mice
Kazuya Matsuo, An Cheng, Yasushi Yabuki, Ibuki Takahata, Hiroyuki Miyachi, Kohji Fukunaga, Neuropharmacology 150, 164-174 (2019). doi: 10.1016/j.neuropharm.2019.03.029
Development of FABP3 ligands that inhibit arachidonic acid-induced α-synuclein oligomerization
An Cheng, Yasuharu Shinoda, Tetsunori Yamamoto, Hiroyuki Miyachi, Kohji Fukunaga, Brain Res. 1707, 190-197 (2019). doi: 10.1016/j.brainres.2018.11.036
Novel indole and benzothiophene ring derivatives showing differential modulatory activity against human epithelial sodium channel subunits, ENaC β and γ
Yoichi Kasahara, Takanobu Sakurai, Ryusei Matsuda, Masataka Narukawa, Akihito Yasuoka, Naoki Mori, Hidenori Watanabe, Takayoshi Okabe, Hirotatsu Kojima, Keiko Abe, Takumi Misaka and Tomiko Asakura, Bioscience, Biotechnology, and Biochemistry, 83, 243-250 (2019).

2018

Development of Pin1 inhibitors and their potential as therapeutic agents
Yusuke Nakatsu, Yasuka Matsunaga, Koji Ueda, Takeshi Yamamotoya, Yuki Inoue, Masa-ki Inoue, Yu Mizuno, Akifumi Kushiyama, Hiraku Ono, Midori Fujishiro, Hisanaka Ito, Takayoshi Okabe, Tomoichiro Asano. Curr Med Chem. 2018 Nov 5. doi: 10.2174/0929867325666181105120911.
東大　化合物ライブラリー
岡部隆義、小島宏建、長野哲雄,ケミカルバイオロジー化合物集オーム社日本学術振興会ケミカルバイオロジー第189委員会編,56-62 (2018).
A small-molecule inhibitor of SOD1-Derlin-1 interaction ameliorates pathology in an ALS mouse model
Naomi Tsuburaya, Kengo Homma, Tsunehiko Higuchi, Andrii Balia, Hiroyuki Yamakoshi, Norio Shibata, Seiichi Nakamura, Hidehiko Nakagawa, Shin-ichi Ikeda, Naoki Umezawa, Nobuki Kato, Satoshi Yokoshima, Masatoshi Shibuya, Manabu Shimonishi, Hirotatsu Kojima, Takayoshi Okabe, Tetsuo Nagano, Isao Naguro, Keiko Imamura, Haruhisa Inoue, Takao Fujisawa, Hidenori Ichijo, Nat. Commun. 9, 2668 (2018)
Discovery of peroxisome proliferator-activated receptor α (PPARα) activators with a ligand-screening system using a human PPARα-expressing cell line
Keisuke Tachibana, Tomohiro Yuzuriha, Ryotaro Tabata, Syohei Fukuda, Takashi Maegawa, Rika Takahashi, Keiichi Tanimoto, Hirofumi Tsujino, Kazuto Nunomura, Bangzhong Lin, Yoshiharu Matsuura, Toshiya Tanaka, Takao Hamakubo, Juro Sakai, Tatsuhiko Kodama, Tadayuki Kobayashi, Kenji Ishimoto, Hiroyuki Miyachi, and Takefumi Doi, J. Biol. Chem. 293, 10333-10343 (2018). doi: 10.1074/jbc.RA118.002077
Inhibitory effects of a novel PPAR-γ agonist MEKT1 on Pomc expression/ACTH secretion in AtT20 cells
Rehana Parvin, Erika Noro, Akiko Saito-Hakoda, Hiroki Shimada, Susumu Suzuki, Kyoko Shimizu, Hiroyuki Miyachi, Atsushi Yokoyama, Akira Sugawara, PPAR Res. 2018, 5346272 (2018). doi: 10.1155/2018/5346272
基礎医学から創薬へ参入の支援
小島宏建, 岡部隆義, 宮地弘幸, 長野哲雄, 生体の科学　69(4), 305-309, (2018).
創薬化学　メディシナルケミストへの道
長野哲雄編, 池田陽介, 河野友昭, 北村吏司, 坂入将夫, 鈴木正則, 須藤直樹著　東京化学同人 (2018).

2017

Discovery of benzo[g]indoles as a novel class of non-covalent Keap1-Nrf2 protein-protein interaction inhibitor
Daisuke Yasuda, Akihiro Yuasa, Rika Obata, Mao Nakajima, Kyoko Takahashi, Yoshinobu Ichimura, Masaaki Komatsu, Masayuki Yamamoto, Riyo Imamura, Hirotatsu Kojima, Takayoshi Okabe, Tetsuo Nagano, Tadahiko Mashino and Tomoyuki Ohe, Bioorg. Med. Chem. Lett., 27, 5006-5009 (2017). doi: 10.1016/j.bmcl.2017.10.008. Epub 2017 Oct 6.
Theoretical Analysis of Activity Cliffs among Benzofuranone-Class Pim1 Inhibitors Using the Fragment Molecular Orbital Method with Molecular Mechanics Poisson-Boltzmann Surface Area (FMO+MM-PBSA) Approach
Chiduru Watanabe , Hirofumi Watanabe, Kaori Fukuzawa, Lorien J. Parker, Yoshio Okiyama, Hitomi Yuki , Shigeyuki Yokoyama, Hirofumi Nakano , Shigenori Tanaka , and Teruki Honma, J. Chem. Inf. Model., 57 (12), pp.2996-3010 (2017).
A proposal for a structural model of the feline calicivirus protease bound to the substrate peptide under physiological conditions
Masaru Yokoyama, Tomoichiro Oka, Hirotaka Takagi, Hirotatsu Kojima, Takayoshi Okabe, Tetsuo Nagano, Yukinobu Tohya and Hironori Sato, Frontiers in Microbiology 8, 1383 (2017).
Norgestimate inhibits staphylococcal biofilm formation and resensitizes methicillin-resistant Staphylococcus aureus to β-lactam antibiotics
Yutaka Yoshii, Ken-ichi Okuda, Satomi Yamada, Mari Nagakura, Shinya Sugimoto, Tetsuo Nagano, Takayoshi Okabe, Hirotatsu Kojima, Takeo Iwamoto, Kazuyoshi Kuwano and Yoshimitsu Mizunoe, npj Biofilms and Microbiomes 3, 18 (2017).
Identification of novel selective P2Y6 receptor antagonists by high-throughput screening assay
Masaaki Ito, Shin-ichiro Egashira, Kazuki Yoshida, Tomoko Mineno, Kazuo Kumagai, Hirotatsu Kojima, Takayoshi Okabe, Tetsuo Nagano, Michio Ui, Isao Matsuoka, Life Sci. 180, 137-142 (2017).
High-throughput Screening of Small Molecule Inhibitors of the Streptococcus Quorum-sensing Signal Pathway
Seiji Ishii, Kenji Fukui, Satoshi Yokoshima, Kazuo Kumagai, Youko Beniyama, Tetsuya Kodama, Tohru Fukuyama, Takayoshi Okabe, Tetsuo Nagano, Hirotatsu Kojima and Takato Yano, Scientific Reports 7, 4029 (2017).
Structural development of 1,2,3,4-tetrahydroisoquinoline-type positive allosteric modulators of prostacyclin receptor (IPPAMs) to improve metabolic stability, and investigation of metabolic fate
Hiroyuki Miyachi, Toshifumi Suzuki, Riyo Imamura, Tetsuo Nagano, Takayoshi Okabe, Bioorganic & Medicinal Chemistry Letters, 27 (15), 3572-3575 (2017).
Synthesis of both enantiomers of 1,2,3,4-tetrahydroisoquinoline derivative IPPAM-1 and enantio-dependency of its positive allosteric modulation of prostacyclin receptor
Kohki Yamamoto, Toshifumi Suzuki, Riyo Imamura, Tetsuo Nagano, Takayoshi Okabe and Hiroyuki Miyachi, Bioorg. Med. Chem. Lett., 27 (11), 2567-2570 (2017). DOI: 10.1016/j.bmcl.2017.03.083
Improving The Solubility of Artificial Ligands of Streptavidin to Enable More Practical Reversible Switching of Protein Localization in Cells
Ryo Tachibana, Takuya Terai, Gaelle Boncompain, Shigeru Sugiyama, Nae Saito, Franck Perez and Yasuteru Urano. ChemBioChem, 18 (4), 358-362 (2017). doi:10.1002/cbic.201600640.
Competitive fragment assay for the selective inhibitor of WNKs kinase
Nae Saito, Yukio Tada, Takayoshi Okabe, Tetsuo Nagano, Chem-Bio Informatics Journal, Vol.17, pp.34-37 (2017).
Design and Synthesis of Potent and Selective PIM Kinase Inhibitors by Targeting Unique Structure of ATP-binding Pocket
Nakano Hirofumi, Hasegawa Tsukasa, Kojima Hirotatsu, Okabe Takayoshi, Nagano Tetsuo. ACS Medicinal Chemistry Letters, 8 (5), 504-509 (2017). doi: 10.1021/acsmedchemlett.6b00518.
Docking simulation of fragment library compounds to find new leads for specific WNK kinase inhibitors
Nae Saito, Yukio Tada, Takayoshi Okabe, Tetsuo Nagano, Chem-Bio Informatics Journal, Vol.17, pp.30-33 (2017).
Discovery and Mechanistic Characterization of Selective Inhibitors of H2S-producing Enzyme: 3-Mercaptopyruvate Sulfurtransferase (3MST) Targeting Active-site Cysteine Persulfide
Kenjiro Hanaoka, Kiyoshi Sasakura, Yusuke Suwanai, Sachiko Toma-Fukai, Kazuhito Shimamoto, Yoko Takano, Norihiro Shibuya, Takuya Terai, Toru Komatsu, Tasuku Ueno, Yuki Ogasawara, Yukihiro Tsuchiya, Yasuo Watanabe, Hideo Kimura, Chao Wang, Masanobu Uchiyama, Hirotatsu Kojima, Takayoshi Okabe, Yasuteru Urano, Toshiyuki Shimizu and Tetsuo Nagano. Scientific Reports, 7, Article 40227 (2017). doi:10.1038/srep40227.
Development of Chemical Tools to Monitor and Control Isoaspartyl Peptide Methyltransferase Activity
Yusuke Kimura, Toru Komatsu, Kouichi Yanagi, Kenjiro Hanaoka, Tasuku Ueno, Takuya Terai, Hirotatsu Kojima, Takayoshi Okabe, Tetsuo Nagano, and Yasuteru Urano, Angew. Chem., Int. Ed., 56 (1), 153-157 (2017). doi:10.1002/anie.201608677.
アカデミア低分子創薬
長野哲雄,「特集号　日本発次世代創薬のための化学」,化学と工業,1月号,pp.14-16 (2017).
第 I 部　新薬創出に向けたプラットフォーム構築　２．オープンイノベーション　１）アカデミアの立場から
小島宏建,岡部隆義,一條秀憲,長野哲雄,医薬ジャーナル増刊号「新薬展望2017」,Vol. 53,pp.23-29 (2017).
アカデミア創薬を牽引する東京大学創薬機構のさらなる基盤構築：東京大学創薬機構構造展開ユニット設立
宮地弘幸,小島宏建,一條秀憲,MEDCHEM NEWS 27(4),178-183 (2017).

2016

An HTRF based high-throughput screening for discovering chemical compounds that inhibit the interaction between Trypanosoma brucei Pex5p and Pex14p
Yuichi Watanabe, Kosuke Kawaguchi, Syuken Saito, Takayoshi Okabe, Kiyoaki Yonesu, Shinichiro Egashira, Masafumi Kameya, Masashi Morita, Yoshinori Kashiwayama, Tsuneo Imanaka. Biochem Biophys Rep. 6, 260-265, (2016).
Synthesis of Keap1-phosphorylated p62 and Keap1-Nrf2 Protein-protein Interaction Inhibitors and Their Inhibitory Activity
Daisuke Yasuda, Mao Nakajima, Akihiro Yuasa, Rika Obata, Kyoko Takahashi, Tomoyuki Ohe, Yoshinobu Ichimura, Masaaki Komatsu, Masayuki Yamamoto, Riyo Imamura, Hirotatsu Kojima, Takayoshi Okabe, Tetsuo Nagano and Tadahiko Mashino Bioorg. Med. Chem. Lett., 26 (24), 5956-5959 (2016).
p62/Sqstm1 Promotes Malignancy of HCV-positive Hepatocellular Carcinoma through Nrf2-dependent Metabolic Reprogramming
Tetsuya Saito, Yoshinobu Ichimura, Keiko Taguchi, Takafumi Suzuki, Tsunehiro Mizushima, Kenji Takagi, Yuki Hirose, Masayuki Nagahashi, Tatsuro Iso, Toshiaki Fukutomi, Maki Ohishi, Keiko Endo, Takefumi Uemura, Yasumasa Nishito, Shujiro Okuda, Miki Obata, Tsuguka Kouno, Riyo Imamura, Yukio Tada, Rika Obata, Daisuke Yasuda, Kyoko Takahashi, Tsutomu Fujimura, Jingbo Pi, Myung-Shik Lee, Takashi Ueno, Tomoyuki Ohe, Tadahiko Mashino, Toshifumi Wakai, Hirotatsu Kojima, Takayoshi Okabe, Tetsuo Nagano, Hozumi Motohashi, Satoshi Waguri, Tomoyoshi Soga, Masayuki Yamamoto, Keiji Tanaka, and Masaaki Komatsu, Nat. Commun., 7, 12030 (2016). doi:10.1038/ncomms12030.
A Novel Diacylglycerol Kinase a-Selective Inhibitor, CU-3 Induces Cancer Cell Apoptosis and EnhancesImmune Response
Ke Liu, Naoko Kunii, Megumi Sakuma, Atsumi Yamaki, Satoru Mizuno, Mayu Sato, Hiromichi Sakai, Sayaka Kado, Kazuo Kumagai, Hirotatsu Kojima, Takayoshi Okabe, Tetsuo Nagano, Yasuhito Shirai and Fumio Sakane, J. Lipid Res., 57, 368-379 (2016). doi:10.1194/jlr.M062794.
Development of a potent and selective FLT3 kinase inhibitor by systematic expansion of a non-selective fragment-screening hit
Hirofumi Nakano, Tsukasa Hasegawa, Riyo Imamura, Nae Saito, Hirotatsu Kojima, Takayoshi Okabe, Tetsuo Nagano., Bioorg. Med. Chem. Lett., 26 (9),2370-2374 (2016).

2015

Supramolecular Ligands for Histone Tails by Employing a Multivalent Display of Trisulfonated Calix[4]arenes
Kimura Yasuaki, Saito Nae, Hanada Kayo, Liu Jiaan, Okabe Takayoshi, Kawashima Shigehiro, Yamatsugu Kenzo, Kanai Motomu. ChemBioChem, 16, 2599-2604 (2015). doi:10.1002/cbic.201500448.
Design and synthesis of an in vivo-efficacious PIM3 kinase inhibitor as a candidate anti-pancreatic cancer agent
Hirofumi Nakano, Tsukasa Hasegawa, Nae Saito, Kaoru Furukawa, Naofumi Mukaida, Hirotatsu Kojima, Takayoshi Okabe, Tetsuo Nagano., Bioorg. Med. Chem. Lett., 25 (24),5687-5693 (2015).
Artificial Ligands of Streptavidin (ALiS): Discovery, Characterization, and Application for Reversible Control of Intracellular Protein Transport
Takuya Terai, Moe Kohno, Gaelle Boncompain, Shigeru Sugiyama, Nae Saito, Ryo Fujikake, Tasuku Ueno, Toru Komatsu, Kenjiro Hanaoka, Takayoshi Okabe, Yasuteru Urano, Franck Perez, and Tetsuo Nagano, J. Am. Chem. Soc., 137 (33),10464-10467 (2015).
A practical fluorogenic substrate for high-throughput screening of glutathione S-transferase inhibitors
Yuuta Fujikawa, Fumika Morisaki, Asami Ogura, Kana Morohashi, Sora Enya, Ryusuke Niwa, Shinji Goto, Hirotatsu Kojima, Takayoshi Okabe, Tetsuo Nagano and Hideshi Inoue, Chem. Commun., 51, 11459-11462 (2015).
Identification of a Dual Inhibitor of SRPK1 and CK2 That Attenuates Pathological Angiogenesis of Macular Degeneration in Mice
Satoshi Morooka, Mitsuteru Hoshina, Isao Kii, Takayoshi Okabe, Hirotatsu Kojima, Naoko Inoue, Yukiko Okuno, Masatsugu Denawa, Suguru Yoshida, Junichi Fukuhara, Kensuke Ninomiya, Teikichi Ikura, Toshio Furuya, Tetsuo Nagano, Kousuke Noda, Susumu Ishida, Takamitsu Hosoya, Nobutoshi Ito, Nagahisa Yoshimura, and Masatoshi Hagiwara, Mol. Pharm. 88, 316-325 (2015).
Gliotoxin Suppresses NF-κB Activation by Selectively Inhibiting Linear Ubiquitin Chain Assembly Complex (LUBAC)
Hiroki Sakamoto, Shinichiro Egashira, Nae Saito, Takayoshi Kirisako, Simon Miller, Yoshiteru Sasaki, Tadahiko Matsumoto, Manabu Shimonishi, Toru Komatsu, Takuya Terai, Tasuku Ueno, Kenjiro Hanaoka, Hirotatsu Kojima, Takayoshi Okabe, Soichi Wakatsuki, Kazuhiro Iwai, and Tetsuo Nagano, ACS Chem. Biol., 10 (3), 675-681 (2015).
特集　創刊50周年記念特集　医薬品開発における産官学連携の展望　２．各論１）東京大学創薬機構の取り組み
小島宏建, 岡部隆義, 一條秀憲, 長野哲雄, 医薬ジャーナル創刊50周年記念特集, Vol.51, 2331-2338 (2015).
創薬スクリーニングに有用な高感度かつ低コストの糖転移酵素およびキナーゼのアッセイ系の開発
熊谷和夫, 小島宏建, 岡部隆義, 長野哲雄, 和光純薬時報, 83(2), 14-17 (2015).

2014

Fluorometric assay of integrin activity with a small-molecular probe that senses the binding site microenvironment
Toru Komatsu, Aoi Takeda, Kenjiro Hanaoka, Takuya Terai, Tasuku Ueno, Yukio Tada, Tetsuo Nagano and Yasuteru Urano, Chem. Commun., 50, 15894-15896 (2014).
High-Throughput Screening System To Identify Small Molecules That Induce Internalization and Degradation of HER2
Masayuki Isa, Daisuke Asanuma, Shigeyuki Namiki, Kazuo Kumagai, Hirotatsu Kojima, Takayoshi Okabe, Tetsuo Nagano, and Kenzo Hirose, ACS Chem. Biol., 9 (10), 2237-2241 (2014).
The DEAH-Box RNA Helicase DHX15 Activates NF-κB and MAPK Signaling Downstream of MAVS During Antiviral Responses
Kenta Mosallanejad, Yusuke Sekine, Seiko Ishikura-Kinoshita, Kazuo Kumagai, Tetsuo Nagano, Atsushi Matsuzawa, Kohsuke Takeda, Isao Naguro and Hidenori Ichijo, Sci. Signal. 7 (323), p. ra40 (2014).
Selective inhibitors of a PAF biosynthetic enzyme lysophosphatidylcholine acyltransferase 2
Megumi Tarui, Hideo Shindou, Kazuo Kumagai, Ryo Morimoto, Takeshi Harayama, Tomomi Hashidate, Hirotatsu Kojima, Takayoshi Okabe, Tetsuo Nagano, Takahide Nagase, Takao Shimizu, J. Lipid Res., 55, 1386-1396 (2014).
Development of a highly sensitive, high-throughput assay for glycosyltransferases using enzyme-coupled fluorescence detection
Kazuo Kumagai, Hirotatsu Kojima, Takayoshi Okabe, Tetsuo Nagano, Analytical Biochemistry, 447, 146-155 (2014).
アカデミアの大規模スクリーニングを可能にするアッセイシステムの開発
熊谷和夫, 長野哲雄, 南山堂, 「生命科学から創薬へのイノベーション」, 米田悦啓, 堤康央, 石井健　編集, 南山堂(2014).
アカデミア創薬を成功させるために
長野哲雄, 堺谷政弘, 実験医学増刊号「研究成果を薬につなげるアカデミア創薬の戦略と実例」, 長野哲雄編集, 32, 158-163 (2014).

2013

Acetaldehyde-induced Cytotoxicity Involves Induction of Spermine Oxidase at Thetranscriptional Level
Takeshi Uemura, Yuka Tanaka, Kyohei Higashi, Daisuke Miyamori, Tomokazu Takasaka,Tetsuo Nagano, Toshihiko Toida, Kanji Yoshimoto, Kazuei Igarashi, Hiroshi Ikegaya, Toxicology, 310, 1-7 (2013).
A small-molecule AdipoR agonist for type 2 diabetes and short life in obesity
Miki Okada-Iwabu, Toshimasa Yamauchi, Masato Iwabu, Teruki Honma, Ken-ichi Hamagami, Koichi Matsuda, Mamiko Yamaguchi, Hiroaki Tanabe, Tomomi Kimura-Someya, Mikako Shirouzu, Hitomi Ogata, Kumpei Tokuyama, Kohjiro Ueki, Tetsuo Nagano, Akiko Tanaka, Shigeyuki Yokoyama, Takashi Kadowaki, Nature, 503, 493-499 (2013).
Identification of Novel Small Compounds that Restore E-cadherin Expression and Inhibit Tumor Cell Motility and Invasiveness
Tamaki Hirano, Reiko Satow, Asami Kato, Mana Tamura, Yumi Murayama, Hideyuki Saya, Hirotatsu Kojima, Tetsuo Nagano, Takayoshi Okabe, Kiyoko Fukami, Biochem. Pharmacol, 86 (10), 1419-1429 (2013).
Screening and X-Ray Crystal Structure-based Optimization of Autotaxin (ENPP2) Inhibitors, Using a Newly Developed Fluorescence Probe
Mitsuyasu Kawaguchi, Takayoshi Okabe, Shinichi Okudaira, Hiroshi Nishimasu, Ryuichiro Ishitani, Hirotatsu Kojima, Osamu Nureki, Junken Aoki, and Tetsuo Nagano, ACS Chemical Biology, 8 (8), 1713-1721 (2013).
Diced electrophoresis gel (DEG) assay for screening enzymes with specified activities
Toru Komatsu, Kenjiro Hanaoka, Alexander Adibekian, Kentaro Yoshioka, Takuya Terai, Tasuku Ueno, Mitsuyasu Kawaguchi, Benjamin F. Cravatt, Tetsuo Nagano, J. Am. Chem. Soc., 135, 6002-6005 (2013).
Oxysterol-binding protein family I is the target of minor enviroxime-like compounds
Minetaro Arita, Hirotatsu Kojima, Tetsuo Nagano, Takayoshi Okabe, Takaji Wakita, Hiroyuki Shimizu, Journal of Virology, 87, 4252-4260 (2013).
A Fluorescence-Based High-Throughput Assay to Identify Small Molecules that Inhibit the Interaction of MdmX with p53
Keiko Tsuganezawa, Yukari Nakagawa, Miki Kato, Shigenao Taruya, Fumio Takahashi, Morio Endoh, Rei Utata, Masumi Mori, Naoko Ogawa, Teruki Honma, Shigeyuki Yokoyama, Yoshinobu Hashizume, Masaaki Aoki, Takuma Kasai, Takanori Kigawa, Hirotatsu Kojima, Takayoshi Okabe, Tetsuo Nagano, Akiko Tanaka, Journal of Biomolecular Screening, 18, 191-198 (2013).
化合物ライブラリーと創薬等支援技術基盤プラットフォーム
小島宏建, 岡部隆義, 長野哲雄, 細胞工学, 32, 638-643 (2013).
創薬オープンイノベーションセンター　―創薬シーズの創製に向けた研究支援ネットワーク―
小島宏建, 岡部隆義, 長野哲雄, 日本薬理学会誌, 141, 327-332 (2013).

2012

Development of NIR Fluorescent Dyes Based on Si-Rhodamine for In Vivo Imaging
Yuichiro Koide, Yasuteru Urano, Kenjiro Hanaoka, Wen Piao, Moriaki Kusakabe, Nae Saito, Takuya Terai, Takayoshi Okabe and Tetsuo Nagano. J. Am. Chem. Soc., 134, 5029-5031 (2012). doi:10.1021/ja210375e.
Identification of novel drug-resistant EGFR mutant inhibitors by in silico screening using comprehensive assessments of protein structures
Tomohiro Sato, Hisami Watanabe, Keiko Tsuganezawa, Hitomi Yuki, Junko Mikuni, Seiko Yoshikawa, Mutsuko Kukimoto-Niino, Takako Fujimoto, Yumiko Terazawa, Motoaki Wakiyama, Hirotatsu Kojima, Takayoshi Okabe, Tetsuo Nagano, Mikako Shirouzu, Shigeyuki Yokoyama, Akiko Tanaka, Teruki Honma, Bioorganic & Medicinal Chemistry, 20 (12), 3756-3767 (2012).
Structural basis for specific recognition of substrates by sapovirus protease
Masaru Yokoyama, Tomoichiro Oka, Hirotatsu Kojima, Tetsuo Nagano, Takayoshi Okabe, Kazuhiko Katayama, Takaji Wakita, Tadahito Kanda, Hironori Sato, Frontiers in Virology, 3, Article312 (2012).
Flexibility of the P-loop of Pim-1 kinase: observation of a novel conformation induced by interaction with an inhibitor
Lorien Parker, HisamiWatanabe, Keiko Tsuganezawa, Yuri Tomabechi, Noriko Handa, Mikako Shirouzu, Hitomi Yuki, Teruki Honma, Naoko Ogawa, Tetsuo Nagano, Shigeyuki Yokoyama, Akiko Tanaka, Acta Cryst., Sec. F Struct. Biol. Cryst. Commun., 68, 860-866 (2012).
Rational evolution of a novel type of potent and selective Proviral Integration site in Moloney murine leukemia kinase 1 (PIM1) inhibitor from a screening-hit compound
Hirofumi Nakano, Nae Saito, Lorien Parker, Yukio Tada, Masanao Abe, Keiko Tsuganezawa, Shigeyuki Yokoyama, Akiko Tanaka, Hirotatsu Kojima, Takayoshi Okabe, Tetsuo Nagano, J. Med. Chem., 55, 5151-5164 (2012).
Blockade of Inflammatory Responses by a Small-Molecule Inhibitor of the Rac Activator DOCK2
Akihiko Nishikimi, Takehito Uruno, Xuefeng Duan, Qinhong Cao, Yuji Okamura, Takashi Saitoh, Nae Saito, Shunsuke Sakaoka, Yao Du, Atsushi Suenaga, Mutsuko Kukimoto-Niino, Kei Miyano, Kazuhito Gotoh, Takayoshi Okabe, Fumiyuki Sanematsu, Yoshihiko Tanaka, Hideki Sumimoto, Teruki Honma, Shigeyuki Yokoyama, Tetsuo Nagano, Daisuke Kohda, Motomu Kanai, Yoshinori Fukui, Chem.& Biol., 19, 488-497 (2012).
A Novel Pim-1 Kinase Inhibitor Targeting Residues That Bind the Substrate Peptide
Keiko Tsuganezawa, Hisami Watanabe, Lorien Parker, Hitomi Yuki, Shigenao Taruya, Yukari Nakagawa, Daisuke Kamei, Masumi Mori, Naoko Ogawa, Yuri Tomabechi, Noriko Handa, Teruki Honma, Shigeyuki Yokoyama, Hirotatsu Kojima, Takayoshi Okabe, Tetsuo Nagano, Akiko Tanaka, J. Mol. Biol., 417, 240-252 (2012).
アカデミア創薬の幕開け－大学で取組む”本格的創薬研究”－
小島宏建, 岡部隆義, 長野哲雄, 現代化学, 500, 26-30 (2012).
公的大規模化合物ライブラリーを基盤とする創薬オープンイノベーション
小島宏建, 岡部隆義, 長野哲雄, 日本臨牀, 70(Suppl 8), 298-302 (2012).
化合物ライブラリーと大量化合物のスクリーニング
小島宏建, 新しい薬学事典朝倉書店笠原忠編, 10-12 (2012).
誰もが使える化合物ライブラリーの構築によるスクリーニングから始める創薬研究の促進
小島宏建, 岡部隆義, 長野哲雄, 実験医学, 30, 1234-1239 (2012).
アカデミアにおける創薬
岡部隆義, 感染・炎症・免疫, 42, 48-57 (2012).

2011

Fluorescence probe for lysophospholipase C/NPP6 activity and a potent NPP6 inhibitor
Mitsuyasu Kawaguchi, Takayoshi Okabe, Shinichi Okudaira, Kenjiro Hanaoka, Yuuta Fujikawa, Takuya Terai, Toru Komatsu, Hirotatsu Kojima, Junken Aoki, Tetsuo Nagano, J. Am. Chem. Soc., 133, 12021-12030 (2011).
Virtual screening and further development of novel ALK inhibitors
Masako Okamoto, Hirotatsu Kojima, Nae Saito, Takayoshi Okabe, Yoshiaki Masuda, Toshio Furuya, Tetsuo Nagano, Bioorganic & Medicinal Chemistry, 19, 3086-3095 (2011).
A dual inhibitor against prolyl isomerase Pin1 and cyclophilin discovered by a novel real-time fluorescence detection method
Tadashi Mori, Masafumi Hidaka, Yi-Chin Lin, Ibuki Yoshizawa, Takayoshi Okabe, Shinichiro Egashira, Hirotatsu Kojima, Tetsuo Nagano, Mamoru Koketsu, Mari Takamiya, Takafumi Uchida, Biochem. Biophys. Res. Comm., 406, 439-443 (2011).
Phosphatidylinositol-4 kinase III beta is a target of enviroxime-like compounds for anti-poliovirus activity
Minetaro Arita, Hirotatsu Kojima, Tetsuo Nagano, Takayoshi Okabe, Takaji Wakita, Hiroyuki Shimizu, J. Virol., 85, 2364-2372 (2011).
Identification of novel ASK1 inhibitors using virtual screening
Masako Okamoto, Nae Saito, Hirotatsu Kojima, Takayoshi Okabe, Kohsuke Takeda, Hidenori Ichijo, Toshio Furuya, Tetsuo Nagano, Bioorganic & Medicinal Chemistry, 19, 486-489 (2011).
化合物ライブラリーを活用した創薬オープンイノベーション
小島宏建, ファルマシア, 47, 729-733 (2011).
創薬研究基盤としての化合物ライブラリーの構築
小島宏建, 岡部隆義, 長野哲雄, 化学工業, 62, 124-130 (2011).

2010

A Time-Resolved Fluorescence Probe for Dipeptidyl Peptidase 4 and its Application for Inhibitor Screening
Mitsuyasu Kawaguchi, Takayoshi Okabe, Takuya Terai, Kenjiro Hanaoka, Hirotatsu Kojima, Izumi Minegishi, Tetsuo Nagano, Chemistry-A European Journal, 16, 13479-13486 (2010).
A Fluorescence Correlation Spectroscopy-based Assay for Fragment Screening of Slowly Inhibiting Protein-peptide Interactions
Junko Mikuni, Miki Kato, Shigenao Taruya, Keiko Tsuganezawa, Masumi Mori, Naoko Ogawa, Teruki Honma, Shigeyuki Yokoyama, Hirotatsu Kojima, Takayoshi Okabe, Tetsuo Nagano, Akiko Tanaka, Analytical Biochemistrey, 402, 26-31 (2010).
Establishment of an indicator cell system for hepatitis C virus
Yoshinori Tanaka, Yoshio Mori, Hideki Tani, Takayuki Abe, Kohji Moriishi, Hirotatsu Kojima, Tetsuo Nagano, Takayoshi Okabe, Tetsuro Suzuki, Masashi Tatsumi, Yoshiharu Matsuura, Microbiol Immunol, 54, 206-220 (2010).

2009

公的化合物ライブラリーの構築と生命科学研究へのインパクト
長野哲雄「MED CHEM NEWS №2」, 19(2), (2009).
融合発展する構造生物学とケミカルバイオロジーの最前線　序
長野哲雄「融合発展する構造生物学とケミカルバイオロジーの最前線」
蛋白質核酸酵素, 54, 1435 (2009).
創薬をめざした構造生物学とケミカルバイオロジーの融合研究
長野哲雄「融合発展する構造生物学とケミカルバイオロジーの最前線」
蛋白質核酸酵素, 54, 1439-1440 (2009).
化合物ライブラリー設備と化合物管理・提供システムの構築
小島宏建「融合発展する構造生物学とケミカルバイオロジーの最前線」
蛋白質核酸酵素, 54, 1512-1517 (2009).
スクリーニング基盤の構築
岡部隆義「融合発展する構造生物学とケミカルバイオロジーの最前線」
蛋白質核酸酵素, 54, 1526-1529 (2009).
ハイスループット細胞アッセイ
岡部隆義「融合発展する構造生物学とケミカルバイオロジーの最前線」
蛋白質核酸酵素, 54, 1563-1567 (2009).
化合物ライブラリーの効率的構築と利用
誌上座談会　ファルマシア, 45, 965-970 (2009).

2008

Development of a Novel Fluorescent Probe for Fluorescence Correlation Spectroscopic Detection of Kinase Inhibitors
Mitsuyasu Kawaguchi, Takuya Terai, Rei Utata, Miki Kato, Keiko Tsuganezawa, Akiko Tanaka, Hirotatsu Kojima, Takayosi Okabe, Tetsuo Nagano, Bioorganic & Medicinal Chemistry Letters, 18, 3752-3755 (2008).
東京大学　生物機能制御化合物ライブラリー機構
ヒューマンサイエンス財団, 「日本国内の創薬ライブラリー資源に関する調査　報告書」,　HSレポート№16, 25-36 (2008).
総長室総括委員会　～東大に生まれる新組織たち～　第5回
長野哲雄, 学内広報, No.1369 14 (2008).
大学における創薬研究に必要な基盤は何か　－大学でなぜ薬が作れないのか－
長野哲雄, 現代化学, 446, 16-19 (2008).
創薬研究には化合物ライブラリーの基盤整備が重要である
長野哲雄, DLM(Drug　Lifetime Management) Center NEWS, 16 (2008).
化合物ライブラリー
長野哲雄, 岡部隆義, 小島宏建, Medical Science Digest, 34(10), 432-433 (2008).