Výsledky vyhledávání - "Tadashi Terasaka"

Discovery of ASP5878: Synthesis and structure-activity relationships of pyrimidine derivatives as pan-FGFRs inhibitors with improved metabolic stability and suppressed hERG channel inhibitory activity

Autor: Ikumi Kuriwaki, Minoru Kameda, Kazuhiko Iikubo, Hiroyuki Hisamichi, Yuichiro Kawamoto, Shigetoshi Kikuchi, Hiroyuki Moritomo, Tadashi Terasaka, Yoshinori Iwai, Atsushi Noda, Hiroshi Tomiyama, Aya Kikuchi, Masaaki Hirano

Publikováno v: Bioorganicmedicinal chemistry. 59

Fibroblast growth factor receptor 3 (FGFR3) is an attractive therapeutic target for the treatment of bladder cancer patients harboring genetic alterations in FGFR3. We identified pyrimidine derivative ASP5878 (27) with improved metabolic stability an

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6b20ff3513887a068ea832036f07ea34
https://pubmed.ncbi.nlm.nih.gov/35219181

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ASP5878, a Novel Inhibitor of FGFR1, 2, 3, and 4, Inhibits the Growth of FGF19-Expressing Hepatocellular Carcinoma

Autor: Tadashi Terasaka, Sadao Kuromitsu, Ayako Nakayama, Tatsuya Kawase, Minoru Kameda, Nobuaki Shindoh, Takashi Futami, Rumi Kihara, Tomoyuki Suzuki, Hidetsugu Okada, Masaaki Hirano

Publikováno v: Molecular Cancer Therapeutics. 16:68-75

Hepatocellular carcinoma is an aggressive cancer with poor prognosis. Fibroblast growth factor 19, a member of the fibroblast growth factor family, is a ligand for fibroblast growth factor receptor 4. Moreover, it plays a crucial role in the progress

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8809ff5174b7efdc90c408235941836a
https://doi.org/10.1158/1535-7163.mct-16-0188

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ASP5878, a selective FGFR inhibitor, to treat FGFR3-dependent urothelial cancer with or without chemoresistance

Autor: Masaaki Hirano, Taisuke Nakazawa, Minoru Kameda, Masateru Iizuka, Aya Kikuchi, Sadao Kuromitsu, Tadashi Terasaka, Tohru Ozawa, Ayako Nakayama, Nobuaki Shindoh, Tomoyuki Suzuki

Publikováno v: Cancer Science

FGF/FGFR gene aberrations such as amplification, mutation and fusion are associated with many types of human cancers including urothelial cancer. FGFR kinase inhibitors are expected to be a targeted therapy for urothelial cancer harboring FGFR3 gene

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0a5a35f4da11aa7d5a8671f496b2b19e
https://pubmed.ncbi.nlm.nih.gov/27885740

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Structural Basis of Compound Recognition by Adenosine Deaminase

Autor: Hiroaki Adachi, Masako Kuno, Isao Nakanishi, Nobuo Seki, Yusuke Mori, Takashi Fujii, K. Takano, Masaichi Warizaya, Hiroyoshi Matsumura, Tsuyoshi Inoue, Tadashi Terasaka, Takayoshi Kinoshita

Publikováno v: Biochemistry. 44:10562-10569

Structural snapshots corresponding to various states enable elucidation of the molecular recognition mechanism of enzymes. Adenosine deaminase has two distinct conformations, an open form and a closed form, although it has so far been unclear what fa

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::44dd2d674db6cad0dd393413320b4412
https://doi.org/10.1021/bi050529e

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Non-nucleoside adenosine deaminase inhibitors: 2000 – 2004

Autor: Tadashi Terasaka

Publikováno v: Expert Opinion on Therapeutic Patents. 15:817-828

Adenosine deaminase (ADA) is a crucial enzyme in purine metabolism that irreversibly deaminates adenosine to form inosine. ADA is ubiquitous in human tissues and plays a crucial role in immune system development. ADA inhibitors may be useful for the

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::3b4af52db70ba8adcabc6227a05481d2
https://doi.org/10.1517/13543776.15.7.817

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Structure-Based Design, Synthesis, and Structure−Activity Relationship Studies of Novel Non-nucleoside Adenosine Deaminase Inhibitors

Autor: Kohichiro Tanaka, Tadashi Terasaka, Masako Kuno, Isao Nakanishi, Nobuo Seki, Takayoshi Kinoshita

Publikováno v: Journal of Medicinal Chemistry. 47:3730-3743

We disclose herein optimization efforts around the novel, highly potent non-nucleoside adenosine deaminase (ADA) inhibitor, 1-[(R)-1-hydroxy-4-(6-(3-(1-methylbenzimidazol-2-yl)propionylamino)indol-1-yl)-2-butyl]imidazole-4-carboxamide 1 (K(i)= 7.7 nM

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ae19b377dbd1e7b261fae59b0c0a4e4a
https://doi.org/10.1021/jm0306374

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