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Design, synthesis, and biological activity of potent and orally available G protein-coupled receptor 40 agonists.
Sasaki S, Kitamura S, Negoro N, Suzuki M, Tsujihata Y, Suzuki N, Santou T, Kanzaki N, Harada M, Tanaka Y, Kobayashi M, Tada N, Funami M, Tanaka T, Yamamoto Y, Fukatsu K, Yasuma T, Momose Y. Sasaki S, et al. Among authors: tsujihata y. J Med Chem. 2011 Mar 10;54(5):1365-78. doi: 10.1021/jm101405t. Epub 2011 Feb 14. J Med Chem. 2011. PMID: 21319751
Identification of fused-ring alkanoic acids with improved pharmacokinetic profiles that act as G protein-coupled receptor 40/free fatty acid receptor 1 agonists.
Negoro N, Sasaki S, Ito M, Kitamura S, Tsujihata Y, Ito R, Suzuki M, Takeuchi K, Suzuki N, Miyazaki J, Santou T, Odani T, Kanzaki N, Funami M, Tanaka T, Yasuma T, Momose Y. Negoro N, et al. Among authors: tsujihata y. J Med Chem. 2012 Feb 23;55(4):1538-52. doi: 10.1021/jm2012968. Epub 2012 Feb 10. J Med Chem. 2012. PMID: 22242551
Discovery of phenylpropanoic acid derivatives containing polar functionalities as potent and orally bioavailable G protein-coupled receptor 40 agonists for the treatment of type 2 diabetes.
Mikami S, Kitamura S, Negoro N, Sasaki S, Suzuki M, Tsujihata Y, Miyazaki T, Ito R, Suzuki N, Miyazaki J, Santou T, Kanzaki N, Funami M, Tanaka T, Yasuma T, Momose Y. Mikami S, et al. Among authors: tsujihata y. J Med Chem. 2012 Apr 26;55(8):3756-76. doi: 10.1021/jm2016123. Epub 2012 Apr 11. J Med Chem. 2012. PMID: 22428944
Optimization of (2,3-dihydro-1-benzofuran-3-yl)acetic acids: discovery of a non-free fatty acid-like, highly bioavailable G protein-coupled receptor 40/free fatty acid receptor 1 agonist as a glucose-dependent insulinotropic agent.
Negoro N, Sasaki S, Mikami S, Ito M, Tsujihata Y, Ito R, Suzuki M, Takeuchi K, Suzuki N, Miyazaki J, Santou T, Odani T, Kanzaki N, Funami M, Morohashi A, Nonaka M, Matsunaga S, Yasuma T, Momose Y. Negoro N, et al. Among authors: tsujihata y. J Med Chem. 2012 Apr 26;55(8):3960-74. doi: 10.1021/jm300170m. Epub 2012 Apr 18. J Med Chem. 2012. PMID: 22490067
Discovery of a novel series of indolinylpyrimidine-based GPR119 agonists: Elimination of ether-a-go-go-related gene liability using a hydrogen bond acceptor-focused approach.
Kamaura M, Kubo O, Sugimoto H, Noguchi N, Miyashita H, Abe S, Matsuda K, Tsujihata Y, Odani T, Iwasaki S, Murata T, Sato K. Kamaura M, et al. Among authors: tsujihata y. Bioorg Med Chem. 2021 Mar 15;34:116034. doi: 10.1016/j.bmc.2021.116034. Epub 2021 Jan 23. Bioorg Med Chem. 2021. PMID: 33548803 Free article.
Discovery of a novel series of GPR119 agonists: Design, synthesis, and biological evaluation of N-(Piperidin-4-yl)-N-(trifluoromethyl)pyrimidin-4-amine derivatives.
Kubo O, Takami K, Kamaura M, Watanabe K, Miyashita H, Abe S, Matsuda K, Tsujihata Y, Odani T, Iwasaki S, Kitazaki T, Murata T, Sato K. Kubo O, et al. Among authors: tsujihata y. Bioorg Med Chem. 2021 Jul 1;41:116208. doi: 10.1016/j.bmc.2021.116208. Epub 2021 May 9. Bioorg Med Chem. 2021. PMID: 34010766 Free article.
Discovery of TAK-875: A Potent, Selective, and Orally Bioavailable GPR40 Agonist.
Negoro N, Sasaki S, Mikami S, Ito M, Suzuki M, Tsujihata Y, Ito R, Harada A, Takeuchi K, Suzuki N, Miyazaki J, Santou T, Odani T, Kanzaki N, Funami M, Tanaka T, Kogame A, Matsunaga S, Yasuma T, Momose Y. Negoro N, et al. Among authors: tsujihata y. ACS Med Chem Lett. 2010 Jun 18;1(6):290-4. doi: 10.1021/ml1000855. eCollection 2010 Sep 9. ACS Med Chem Lett. 2010. PMID: 24900210 Free PMC article.
TAK-875, an orally available G protein-coupled receptor 40/free fatty acid receptor 1 agonist, enhances glucose-dependent insulin secretion and improves both postprandial and fasting hyperglycemia in type 2 diabetic rats.
Tsujihata Y, Ito R, Suzuki M, Harada A, Negoro N, Yasuma T, Momose Y, Takeuchi K. Tsujihata Y, et al. J Pharmacol Exp Ther. 2011 Oct;339(1):228-37. doi: 10.1124/jpet.111.183772. Epub 2011 Jul 13. J Pharmacol Exp Ther. 2011. PMID: 21752941
24 results