Zobrazeno 1 - 10
of 47
pro vyhledávání: '"Bi‐Ching Sang"'
Autor:
Fukuda Hiromi, Weston Lane, Shinichiro Matsunaga, Masayuki Gotoh, Tomohiro Kawamoto, Masashi Takahashi, Seiji Miwatashi, Sachiko Itono, Rei Okamoto, Satoko Unno, Kengo Okada, Takahiro Miyazaki, Toshimasa Tanaka, Hiroshi Sugimoto, Kumar Singh Saikatendu, Akira Kaieda, Yuri Hori, Terufumi Takagi, Shinji Morimoto, Bi-Ching Sang
Publikováno v:
ChemMedChem. 14:2093-2101
We identified novel potent inhibitors of p38 mitogen-activated protein (MAP) kinase using a structure-based design strategy, beginning with lead compound, 3-(butan-2-yl)-6-(2,4-difluoroanilino)-1,3-dihydro-2H-imidazo[4,5-b]pyridin-2-one (1). To enhan
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d06cf5c82221bd484b2152ab4bf618c9
https://doi.org/10.1002/cmdc.201900373
https://doi.org/10.1002/cmdc.201900373
Autor:
Osamu Kurasawa, Yasutomi Asano, Ke Li, Hiroshi Banno, Jun Fujimoto, Georgia Kefala, Gyorgy Snell, Irena Levin, Takuto Kojima, Ryo Mizojiri, Bi-Ching Sang, Richard Tjhen, Michael G. Klein, Scott Weston Lane, Isaac Hoffman, Tsuyoshi Ishii, Douglas R. Cary, Xin Liu, Akito Hata, Tadahiro Nambu, Yasuyuki Debori, Tomoya Sameshima, Terufumi Takagi, Steve C. Ding, Akito Nakamura, Maki Miyamoto
Publikováno v:
ACS Med Chem Lett
[Image: see text] General control nonderepressible 2 (GCN2) is a master regulator kinase of amino acid homeostasis and important for cancer survival in the tumor microenvironment under amino acid depletion. We initiated studies aiming at the discover
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::662a272fad1883740a1bb55324dbb6d0
https://doi.org/10.1021/acsmedchemlett.9b00400
https://doi.org/10.1021/acsmedchemlett.9b00400
Autor:
Akira Kaieda, Masashi Takahashi, Hiromi Fukuda, Rei Okamoto, Shinji Morimoto, Masayuki Gotoh, Takahiro Miyazaki, Yuri Hori, Satoko Unno, Tomohiro Kawamoto, Toshimasa Tanaka, Sachiko Itono, Terufumi Takagi, Hiroshi Sugimoto, Kengo Okada, Gyorgy Snell, Ryan Bertsch, Jasmine Nguyen, Bi‐Ching Sang, Seiji Miwatashi
Publikováno v:
ChemMedChem. 14:1022-1030
We identified a lead series of p38 mitogen-activated protein kinase inhibitors using a structure-based design strategy from high-throughput screening of hit compound 1. X-ray crystallography of 1 with the kinase showed an infrequent flip of the pepti
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8b4b80ee91301d96aac6b39f1b699278
https://doi.org/10.1002/cmdc.201900129
https://doi.org/10.1002/cmdc.201900129
Autor:
Ryokichi Koyama, Geza Ambrus-Aikelin, Darbi Witmer, Bi-Ching Sang, Yasunori Fukuda, Hidehisa Iwata, Hideyuki Nakagawa, Masaharu Nakayama, Yusuke Kamada
Publikováno v:
ASSAY and Drug Development Technologies. 16:194-204
The retinoic acid-related orphan receptor gamma T (RORγt) plays an important role in Th17 cell proliferation and functionality. Thus, RORγt inverse agonists are thought to be potent therapeutic agents for Th17-mediated autoimmune diseases, such as
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::59d9bc10dbf1390655dbeac60d89a052
https://doi.org/10.1089/adt.2018.852
https://doi.org/10.1089/adt.2018.852
Autor:
Junya Shirai, Yoshiyuki Fukase, Keiko Koga, Ryoukichi Koyama, Hideyuki Nakagawa, Isaac Hoffman, Bi-Ching Sang, Mitsunori Kono, Toshitake Okui, Satoshi Yamamoto, Yasushi Fujitani, Masaharu Nakayama, Yoshihide Tomata, Robert J. Skene, Kazuko Yonemori, Atsuko Ochida, Masashi Yamasaki, Ayumu Sato
Publikováno v:
Bioorganic & Medicinal Chemistry. 26:721-736
Novel small molecules were synthesized and evaluated as retinoic acid receptor-related orphan receptor-gamma t (RORγt) inverse agonists for the treatment of inflammatory and autoimmune diseases. A hit compound, 1, was discovered by high-throughput s
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5c0bcec89232f743c17ead49dd6e7d73
https://doi.org/10.1016/j.bmc.2017.12.039
https://doi.org/10.1016/j.bmc.2017.12.039
Autor:
Masashi Yamasaki, Ayumu Sato, Tsuneo Oda, Gyorgy Snell, Junya Shirai, Yoshiyuki Fukase, Bi-Ching Sang, Keiko Uga, Atsuko Ochida, Yusuke Sasaki, Hideyuki Nakagawa, Akira Shibata, Satoshi Yamamoto, Naoki Ishii, Yoshihide Tomata, Shoji Fukumoto, Mikio Shirasaki, Isaac Hoffman, Mitsunori Kono, Robert J. Skene, Yumi N. Imai
Publikováno v:
ChemMedChem. 14(22)
Retinoic-acid-related orphan receptor γt (RORγt) inverse agonists could be used for the treatment of autoimmune diseases. Previously, we reported a novel quinazolinedione 1 a with a flexible linear linker as a novel RORγt inverse agonist. A U-shap
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c774a9c6a16ee109cae218661d3aa241
https://pubmed.ncbi.nlm.nih.gov/31659845
https://pubmed.ncbi.nlm.nih.gov/31659845
Autor:
Naohiro Taya, Chien-Hung Chen, Tsuneo Oda, Bi-Ching Sang, Tomoya Yukawa, Takayuki Sato, Yoshi Nara, Noriko Uchiyama, Zenyu Shiokawa, Terufumi Takagi, Satoshi Yamamoto, Ayumu Sato, Ryokichi Koyama, Nobuyuki Negoro, Gyorgy Snell, Junya Shirai, Ryosuke Katsuyama, Takashi Imada, Yoshihiro Banno, Isaac Hoffman, Tetsuji Kawamoto, Mitsunori Kono, Robert J. Skene
Publikováno v:
Journal of medicinal chemistry. 62(3)
Retinoic acid receptor-related orphan receptor γt (RORγt) agonists are expected to provide a novel class of immune-activating anticancer drugs via activation of Th17 cells and Tc17 cells. Herein, we describe a novel structure-based functionality sw
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1871e7ef2034f04a5ead2918edf01322
https://pubmed.ncbi.nlm.nih.gov/30652849
https://pubmed.ncbi.nlm.nih.gov/30652849
Autor:
Michael G. Klein, Taisuke Katoh, Etsurou Watanabe, Gyorgy Snell, Yoshihisa Nakada, Hideyuki Nakagawa, Tetsuya Tsukamoto, Takeo Arita, Hiroki Hayashi, Bi-Ching Sang, Takafumi Takai, Hua Zou, Hideyuki Mototani, Takafumi Yukawa
Publikováno v:
Bioorganic & Medicinal Chemistry. 24(11):2466-2475
A high-throughput screening campaign helped us to identify an initial lead compound (1) as a protein kinase C-θ (PKCθ) inhibitor. Using the docking model of compound 1 bound to PKCθ as a model, structure-based drug design was employed and two regi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9d7c481e52e640dfa35f76809f09cd3e
Autor:
Keiko Igaki, Yoshihiro Banno, Tsuneo Oda, Akira Shibata, Bi-Ching Sang, Masashi Yamasaki, Hideyuki Nakagawa, Atsuko Ochida, Hidekazu Tokuhara, Kazuko Yonemori, Junya Shirai, Satoshi Yamamoto, Yoshiyuki Fukase, Gyorgy Snell, Shinichi Masada, Tomoya Yukawa, Yoshi Nara, Isaac Hoffman, Tetsuji Kawamoto, Mitsunori Kono, Noboru Tsuchimori, Yoshiki Nakamura, Keiko Uga, Takashi Imada, Naohiro Taya, Robert J. Skene
Publikováno v:
Journal of medicinal chemistry. 61(7)
A series of tetrahydronaphthyridine derivatives as novel RORγt inverse agonists were designed and synthesized. We reduced the lipophilicity of tetrahydroisoquinoline compound 1 by replacement of the trimethylsilyl group and SBDD-guided scaffold exch
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9548ec5d97f7b04e014802ee8f90a5b0
https://pubmed.ncbi.nlm.nih.gov/29510038
https://pubmed.ncbi.nlm.nih.gov/29510038
Autor:
Ryoukichi Koyama, Geza Ambrus-Aikelin, Hideyuki Nakagawa, Satoshi Yamamoto, Masaharu Nakayama, Junya Shirai, Bi-Ching Sang, Atsuko Ochida, Yusuke Kamada, Mitsunori Kono
Publikováno v:
Pharmacology. 102(5-6)
Background/Aims: Retinoid-related orphan receptor gamma t (RORγt) is a master regulator of T helper 17 cells that plays a pivotal role in the production of inflammatory cytokines including interleukin (IL)-17. Therefore, RORγt has attracted much at
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e01f8f36fc87c5de90008ec945ff7253
https://pubmed.ncbi.nlm.nih.gov/30134246
https://pubmed.ncbi.nlm.nih.gov/30134246