Research
Faculty Members
Drug Innovation Center Lead Exploration Unit
Kitazaki TomoyukiSpecially Appointed Assosiate Professor
I will contribute to drug discovery originating from academia by utilizing my experience as a medicinal chemist at the pharmaceutical company. I will operate the BINDS (Basis for Supporting Innovative Drug Discovery and Life Science Research) system at the Center for supporting Drug Discovery and Life Science Research of the Graduate School of Pharmaceutical Sciences and support the drug discovery research nationwide.
Education:
1987 M.S. (Synthetic Chemistry) Kyusyu University
2000 Ph.D (Engineering) Kyusyu University
Work Experience:
1987 Takeda Pharmaceutical Company Ltd.
2017 Axcelead Drug Discovery Partners Inc.
2022 Lead Exploration Units, Graduate School of Pharmaceutical Science, Osaka University
Awards:
2006 Breakthrough Award, Division of Medicinal Chemistry, The Pharmaceutical Society of Japan
Research theme
Drug discovery support based on academic seeds, etc.
In order to develop academic seeds into potential pharmaceutical products, I support drug discovery research by utilizing the knowledge and skills accumulated in pharmaceutical companies.
1.Identifying issues faced by clients through consulting and providing solutions through BINDS support
2.Expanding collaboration within and outside BINDS to provide more effective research support
3.Outreach activities to expand BINDS support
Representative achievements
Discovery of a novel series of medium-sized cyclic enteropeptidase inhibitors
Fumiaki Kikuchi, Zenichi Ikeda, Keiko Kakegawa, Youichi Nishikawa, Shigekazu Sasaki, Koichiro Fukuda, Kazuaki Takami, Yoshihiro Banno, Hitoaki Nishikawa, Naohiro Taya, Takashi Nakahata, Sachiko Itono, Hiroaki Yashiro, Kazue Tsuchimori, Hideyuki Hiyoshi, Masako Sasaki, Kimio Tohyama, Kouta Matsumiya, Youko Ishihara, Tetsuji Kawamoto, Masahiro Kamaura, Masanori Watanabe, Tomoyuki Kitazaki, Tsuyoshi Maekawa, Minoru Sasaki
Bioorg. Med. Chem. 2023, 93, 117462-117479.
Design, Synthesis, and Biological Evaluation of a Novel Series of 4‑Guanidinobenzoate Derivatives as Enteropeptidase Inhibitors with Low Systemic Exposure for the Treatment of Obesity
Zenichi Ikeda, Keiko Kakegawa, Fumiaki Kikuchi, Sachiko Itono, Hideyuki Oki, Hiroaki Yashiro, Hideyuki Hiyoshi, Kazue Tsuchimori, Kenichi Hamagami, Masanori Watanabe, Masako Sasaki, Youko Ishihara, Kimio Tohyama, Tomoyuki Kitazaki, Tsuyoshi Maekawa, and Minoru Sasaki
J. Med. Chem. 2022, 65, 8456-8477.
Discovery of a novel series of GPR119 agonists: Design, synthesis, and biological evaluation of N-(Piperidin-4-yl)-N-(trifluoromethyl) pyrimidin-4-amine derivatives
Osamu Kubo, Kazuaki Takami, Masahiro Kamaura, Koji Watanabe, Hirohisa Miyashita, Shinichi Abe, Kae Matsuda, Yoshiyuki Tsujihata, Tomoyuki Odani, Shinji Iwasaki, Tomoyuki Kitazaki, Toshiki Murata, Kenjiro Sato
Bioorg. Med. Chem. 2021, 41, 116208-116221.
Inhibition of MGAT2 modulates fat-induced gut peptide release and fat intake in normal mice and ameliorates obesity and diabetes in ob/ob mice fed on a high-fat diet
Taisuke Mochida, Kazumi Take, Toshiyuki Maki, Masanori Nakakariya, Ryutaro Adachi, Kenjiro Sato, Tomoyuki Kitazaki, Shiro Takekawa
FEBS Open Bio 10(2020) 316-326.
Pharmacological inhibition of monoacylglycerol o-Acyltransferase 2 improves hyperlipidemia, obesity, and diabetes by change in intestinal fat utilization
Kazumi Take, Taisuke Mochida, Toshiyuki Maki, Yoshinori Satomi, Megumi Hirayama, Masanori Nakakariya, Nobuyuki Amano, Ryutaro Adachi, Kenjiro Sato, Tomoyuki Kitazaki, Shiro Takekawa
PLoS ONE 2016; 11(3), 1-18.
Optimization of a novel series of N-phenylindoline-5-sulfonamide-based acyl CoA:monoacylglycerol acyltransferase-2 inhibitors: Mitigation of CYP3A4 time-dependent inhibition and phototoxic liabilities
Kenjiro Sato, Hiroki Takahagi, Osamu Kubo, Kousuke Hidaka, Takeshi Yoshikawa, Masahiro Kamaura, Masanori Nakakariya, Nobuyuki Amano, Ryutaro Adachi, Toshiyuki Maki, Kazumi Take, Shiro Takekawa, Tomoyuki Kitazaki, Tsuyoshi Maekawa
Bioorg. Med. Chem. 2015, 23, 4544-4560.
Discovery of a Novel Series of N‑Phenylindoline-5-sulfonamide Derivatives as Potent, Selective, and Orally Bioavailable Acyl CoA:Monoacylglycerol Acyltransferase‑2 Inhibitors
Kenjiro Sato, Hiroki Takahagi, Takeshi Yoshikawa, Shinji Morimoto, Takafumi Takai, Kousuke Hidaka, Masahiro Kamaura, Osamu Kubo, Ryutaro Adachi, Tsuyoshi Ishii, Toshiyuki Maki, Taisuke Mochida, Shiro Takekawa, Masanori Nakakariya, Nobuyuki Amano, and Tomoyuki Kitazaki
J. Med. Chem. 2015, 58, 3892-3909.
Discovery of 1-{4-[1-(2,6-Difluorobenzyl)-5-[(dimethylamino)methyl]-3-(6-methoxypyridazin-3-yl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl]phenyl}-3-methoxyurea (TAK-385) as a Potent, Orally Active, Non-Peptide Antagonist of the Human Gonadotropin-Releasing Hormone Receptor
Kazuhiro Miwa, Takenori Hitaka, Takashi Imada, Satoshi Sasaki, Mie Yoshimatsu, Masami Kusaka, Akira Tanaka, Daisuke Nakata, Shuichi Furuya, Satoshi Endo, Kazumasa Hamamura, and Tomoyuki Kitazaki
J. Med. Chem. 2011, 54, 4998-5012.
A novel cyclohexene derivative, ethyl (6R)-6-[N-(2-chloro-4-fluorophenyl) sulfamoyl]cyclohex-1-ene-1-carboxylate (TAK-242), selectively inhibits toll-like receptor 4-mediated cytokine production through suppression of intracellular signaling
Masayuki Ii, Naoko Matsunaga, Kaoru Hazeki, Kazuyo Nakamura, Katsunori Takashima, Tsukasa Seya, Osamu Hazeki, Tomoyuki Kitazaki, Yuji Iizawa
Molecular Pharmacology 2006, 69(4) 1288-1295.
Discovery of Novel and Potent Small-Molecule Inhibitors of NO and Cytokine Production as Antisepsis Agents: Synthesis and Biological Activity of Alkyl 6-(N-Substituted sulfamoyl)cyclohex-1-ene-1-carboxylate
Masami Yamada, Takashi Ichikawa, Masayuki Ii, Mie Sunamoto, Katsumi Itoh, Norikazu Tamura, and Tomoyuki Kitazaki
J. Med. Chem. 2005, 48, 7457-7467.