Výsledky vyhledávání - "Takahide Ohishi"

Novel GPR119 agonist AS1669058 potentiates insulin secretion from rat islets and has potent anti-diabetic effects in ICR and diabetic db/db mice

Autor: Yasuo Uchiyama, Yasuhiro Yonetoku, Hirotsugu Tanaka, Takahide Ohishi, Hiroyuki Oshima, Shigeru Yoshida, Tetsuo Matsui, Masayuki Shibasaki

Publikováno v: Life Sciences. 92:167-173

Aims G-protein-coupled receptor 119 (GPR119), mainly expressed in pancreatic β-cells, represents a new target for treating type 2 diabetes. GPR119 agonist is known to induce insulin secretion in a glucose-dependent manner by elevating intracellular

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bad2646b34eefcdfa9dcbdcd2ed4bc1b
https://doi.org/10.1016/j.lfs.2012.11.015

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The therapeutic potential of GPR119 agonists for type 2 diabetes

Autor: Shigeru Yoshida, Takahide Ohishi

Publikováno v: Expert Opinion on Investigational Drugs. 21:321-328

Patients with type 2 diabetes mellitus (T2DM) are reaching an explosive number. Pancreatic β cell dysfunction is the characteristic feature of the progression of T2DM and there is an increasing need for agents to improve its function. GPR119 is a G

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7d92686918591425f0603efbe1c83c2d
https://doi.org/10.1517/13543784.2012.657797

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The role of small molecule GPR119 agonist, AS1535907, in glucose-stimulated insulin secretion and pancreatic β-cell function

Autor: Tetsuo Matsui, Hirotsugu Tanaka, Satoshi Yoshida, Masayuki Shibasaki, Takahide Ohishi, Yasuhiro Yonetoku, Hiroyuki Oshima

Publikováno v: Diabetes, Obesity and Metabolism. 13:34-41

Aim: AS1535907, a small molecule agonist of GPR119, was assessed for its glucose-stimulated insulin secretory activity and pancreatic β-cell function in type 2 diabetes. Methods: Both in vitro and in vivo tests were conducted using NIT-1 and HEK293

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::76fe9402c6298729a6874fedef7a3a41
https://doi.org/10.1111/j.1463-1326.2010.01315.x

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Novel GPR119 agonist AS1535907 contributes to first-phase insulin secretion in rat perfused pancreas and diabetic db/db mice

Autor: Hirotsugu Tanaka, Masayuki Shibasaki, Yasuhiro Yonetoku, Takahide Ohishi, Shigeru Yoshida, Hiroyuki Oshima, Tetsuo Matsui

Publikováno v: Biochemical and Biophysical Research Communications. 402:280-285

G protein-coupled receptor (GPR) 119 is highly expressed in pancreatic β-cells and enhances the effect of glucose-stimulated insulin secretion (GSIS) on activation. The development of an oral GPR119 agonist that specifically targets the first phase

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::259ba6df4687fae7e346a9c3ff11e20e
https://doi.org/10.1016/j.bbrc.2010.10.015

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A selective PIKfyve inhibitor blocks PtdIns(3,5)P 2 production and disrupts endomembrane transport and retroviral budding

Autor: Masahiko Hayakawa, Paul Workman, Harold B. J. Jefferies, Hiroyuki Kaizawa, Tomonobu Koizumi, Christine Boucheron, Michael D. Waterfield, Takahide Ohishi, Peter J. Parker, Parmjit S. Jat, Frank T. Cooke

Publikováno v: EMBO Reports

Phosphoinositides have crucial roles in cellular controls, many of which have been established through the use of small-molecule inhibitors. Here, we describe YM201636, a potent inhibitor of the mammalian class III phosphatidylinositol phosphate kina

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::96c5e878f8aaec00c938c57efc82253b
https://doi.org/10.1038/sj.embor.7401155

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Synthesis and biological evaluation of sulfonylhydrazone-substituted imidazo[1,2-a]pyridines as novel PI3 kinase p110α inhibitors

Autor: Hiroyuki Kaizawa, Kenichi Kawaguchi, Michael D. Waterfield, Mitsuaki Ohta, Mayumi Yamano, Tomonobu Koizumi, Takahide Ohishi, Shin-ichi Tsukamoto, Florence I. Raynaud, Masahiko Hayakawa, Minoru Okada, Peter J. Parker, Paul Workman

Publikováno v: Bioorganic & Medicinal Chemistry. 15:5837-5844

We have previously reported the imidazo[1,2-a]pyridine derivative 4 as a novel p110alpha inhibitor; however, although 4 is a potent inhibitor of p110alpha enzymatic activity and tumor cell proliferation in vitro, it is unstable in solution and ineffe

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1f5e548adcd41ccd152eeb10aa0a9612
https://doi.org/10.1016/j.bmc.2007.05.070

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Synthesis and biological evaluation of imidazo[1,2-a]pyridine derivatives as novel PI3 kinase p110α inhibitors

Autor: Hiroyuki Kaizawa, Masahiko Hayakawa, Florence I. Raynaud, Shin-ichi Tsukamoto, Paul Workman, Peter J. Parker, Minoru Okada, Noriko Ishikawa, Tomonobu Koizumi, Michael D. Waterfield, Takahide Ohishi, Kenichi Kawaguchi, Mayumi Yamano, Mitsuaki Ohta

Publikováno v: Bioorganic & Medicinal Chemistry. 15:403-412

3-{1-[(4-Fluorophenyl)sulfonyl]-1H-pyrazol-3-yl}-2-methylimidazo[1,2-a]pyridine, 2a, was discovered in our chemical library as a novel p110alpha inhibitor with an IC(50) of 0.67microM, through screening in a scintillation proximity assay. Optimizatio

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::dc52d040493ea975b2dd9e89b723b37e
https://doi.org/10.1016/j.bmc.2006.09.047

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