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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: ito r, ito m. J Med Chem. 2012 Apr 26;55(8):3960-74. doi: 10.1021/jm300170m. Epub 2012 Apr 18. J Med Chem. 2012. PMID: 22490067
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: ito r, ito m. 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 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: ito r, ito m. 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.
Discovery of selective ATP-competitive eIF4A3 inhibitors.
Ito M, Iwatani M, Kamada Y, Sogabe S, Nakao S, Tanaka T, Kawamoto T, Aparicio S, Nakanishi A, Imaeda Y. Ito M, et al. Bioorg Med Chem. 2017 Apr 1;25(7):2200-2209. doi: 10.1016/j.bmc.2017.02.035. Epub 2017 Feb 20. Bioorg Med Chem. 2017. PMID: 28283335
Discovery of 3-Benzyl-1-( trans-4-((5-cyanopyridin-2-yl)amino)cyclohexyl)-1-arylurea Derivatives as Novel and Selective Cyclin-Dependent Kinase 12 (CDK12) Inhibitors.
Ito M, Tanaka T, Toita A, Uchiyama N, Kokubo H, Morishita N, Klein MG, Zou H, Murakami M, Kondo M, Sameshima T, Araki S, Endo S, Kawamoto T, Morin GB, Aparicio SA, Nakanishi A, Maezaki H, Imaeda Y. Ito M, et al. J Med Chem. 2018 Sep 13;61(17):7710-7728. doi: 10.1021/acs.jmedchem.8b00683. Epub 2018 Aug 20. J Med Chem. 2018. PMID: 30067358
In Vivo Knockdown of Pathogenic Proteins via Specific and Nongenetic Inhibitor of Apoptosis Protein (IAP)-dependent Protein Erasers (SNIPERs).
Ohoka N, Okuhira K, Ito M, Nagai K, Shibata N, Hattori T, Ujikawa O, Shimokawa K, Sano O, Koyama R, Fujita H, Teratani M, Matsumoto H, Imaeda Y, Nara H, Cho N, Naito M. Ohoka N, et al. Among authors: ito m. J Biol Chem. 2017 Mar 17;292(11):4556-4570. doi: 10.1074/jbc.M116.768853. Epub 2017 Feb 2. J Biol Chem. 2017. PMID: 28154167 Free PMC article.
Discovery of Allosteric Inhibitors Targeting the Spliceosomal RNA Helicase Brr2.
Iwatani-Yoshihara M, Ito M, Klein MG, Yamamoto T, Yonemori K, Tanaka T, Miwa M, Morishita D, Endo S, Tjhen R, Qin L, Nakanishi A, Maezaki H, Kawamoto T. Iwatani-Yoshihara M, et al. Among authors: ito m. J Med Chem. 2017 Jul 13;60(13):5759-5771. doi: 10.1021/acs.jmedchem.7b00461. Epub 2017 Jun 20. J Med Chem. 2017. PMID: 28586220
Derivatization of inhibitor of apoptosis protein (IAP) ligands yields improved inducers of estrogen receptor α degradation.
Ohoka N, Morita Y, Nagai K, Shimokawa K, Ujikawa O, Fujimori I, Ito M, Hayase Y, Okuhira K, Shibata N, Hattori T, Sameshima T, Sano O, Koyama R, Imaeda Y, Nara H, Cho N, Naito M. Ohoka N, et al. Among authors: ito m. J Biol Chem. 2018 May 4;293(18):6776-6790. doi: 10.1074/jbc.RA117.001091. Epub 2018 Mar 15. J Biol Chem. 2018. PMID: 29545311 Free PMC article.
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