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Molecular mechanism and potential target indication of TAK-931, a novel CDC7-selective inhibitor.
Iwai K, Nambu T, Dairiki R, Ohori M, Yu J, Burke K, Gotou M, Yamamoto Y, Ebara S, Shibata S, Hibino R, Nishizawa S, Miyazaki T, Homma M, Oguro Y, Imada T, Cho N, Uchiyama N, Kogame A, Takeuchi T, Kurasawa O, Yamanaka K, Niu H, Ohashi A. Iwai K, et al. Among authors: miyazaki t. Sci Adv. 2019 May 22;5(5):eaav3660. doi: 10.1126/sciadv.aav3660. eCollection 2019 May. Sci Adv. 2019. PMID: 31131319 Free PMC article.
Discovery of a Novel, Highly Potent, and Selective Thieno[3,2-d]pyrimidinone-Based Cdc7 Inhibitor with a Quinuclidine Moiety (TAK-931) as an Orally Active Investigational Antitumor Agent.
Kurasawa O, Miyazaki T, Homma M, Oguro Y, Imada T, Uchiyama N, Iwai K, Yamamoto Y, Ohori M, Hara H, Sugimoto H, Iwata K, Skene R, Hoffman I, Ohashi A, Nomura T, Cho N. Kurasawa O, et al. Among authors: miyazaki t. J Med Chem. 2020 Feb 13;63(3):1084-1104. doi: 10.1021/acs.jmedchem.9b01427. Epub 2020 Jan 14. J Med Chem. 2020. PMID: 31895562
Identification of a new class of potent Cdc7 inhibitors designed by putative pharmacophore model: Synthesis and biological evaluation of 2,3-dihydrothieno[3,2-d]pyrimidin-4(1H)-ones.
Kurasawa O, Oguro Y, Miyazaki T, Homma M, Mori K, Iwai K, Hara H, Skene R, Hoffman I, Ohashi A, Yoshida S, Ishikawa T, Cho N. Kurasawa O, et al. Among authors: miyazaki t. Bioorg Med Chem. 2017 Apr 1;25(7):2133-2147. doi: 10.1016/j.bmc.2017.02.021. Epub 2017 Feb 16. Bioorg Med Chem. 2017. PMID: 28284870
CLK-dependent exon recognition and conjoined gene formation revealed with a novel small molecule inhibitor.
Funnell T, Tasaki S, Oloumi A, Araki S, Kong E, Yap D, Nakayama Y, Hughes CS, Cheng SG, Tozaki H, Iwatani M, Sasaki S, Ohashi T, Miyazaki T, Morishita N, Morishita D, Ogasawara-Shimizu M, Ohori M, Nakao S, Karashima M, Sano M, Murai A, Nomura T, Uchiyama N, Kawamoto T, Hara R, Nakanishi O, Shumansky K, Rosner J, Wan A, McKinney S, Morin GB, Nakanishi A, Shah S, Toyoshiba H, Aparicio S. Funnell T, et al. Among authors: miyazaki t. Nat Commun. 2017 Feb 23;8(1):7. doi: 10.1038/s41467-016-0008-7. Nat Commun. 2017. PMID: 28232751 Free PMC article.
Design and synthesis of novel DFG-out RAF/vascular endothelial growth factor receptor 2 (VEGFR2) inhibitors: 2. Synthesis and characterization of a novel imide-type prodrug for improving oral absorption.
Okaniwa M, Imada T, Ohashi T, Miyazaki T, Arita T, Yabuki M, Sumita A, Tsutsumi S, Higashikawa K, Takagi T, Kawamoto T, Inui Y, Yoshida S, Ishikawa T. Okaniwa M, et al. Among authors: miyazaki t. Bioorg Med Chem. 2012 Aug 1;20(15):4680-92. doi: 10.1016/j.bmc.2012.06.015. Epub 2012 Jun 15. Bioorg Med Chem. 2012. PMID: 22763369
Design and synthesis of novel DFG-out RAF/vascular endothelial growth factor receptor 2 (VEGFR2) inhibitors: 3. Evaluation of 5-amino-linked thiazolo[5,4-d]pyrimidine and thiazolo[5,4-b]pyridine derivatives.
Hirose M, Okaniwa M, Miyazaki T, Imada T, Ohashi T, Tanaka Y, Arita T, Yabuki M, Kawamoto T, Tsutsumi S, Sumita A, Takagi T, Sang BC, Yano J, Aertgeerts K, Yoshida S, Ishikawa T. Hirose M, et al. Among authors: miyazaki t. Bioorg Med Chem. 2012 Sep 15;20(18):5600-15. doi: 10.1016/j.bmc.2012.07.032. Epub 2012 Jul 23. Bioorg Med Chem. 2012. PMID: 22883026
Design and synthesis of novel DFG-out RAF/vascular endothelial growth factor receptor 2 (VEGFR2) inhibitors. 1. Exploration of [5,6]-fused bicyclic scaffolds.
Okaniwa M, Hirose M, Imada T, Ohashi T, Hayashi Y, Miyazaki T, Arita T, Yabuki M, Kakoi K, Kato J, Takagi T, Kawamoto T, Yao S, Sumita A, Tsutsumi S, Tottori T, Oki H, Sang BC, Yano J, Aertgeerts K, Yoshida S, Ishikawa T. Okaniwa M, et al. Among authors: miyazaki t. J Med Chem. 2012 Apr 12;55(7):3452-78. doi: 10.1021/jm300126x. Epub 2012 Mar 14. J Med Chem. 2012. PMID: 22376051
Discovery of Novel and Potent Stearoyl Coenzyme A Desaturase 1 (SCD1) Inhibitors as Anticancer Agents.
Imamura K, Tomita N, Kawakita Y, Ito Y, Ono K, Nii N, Miyazaki T, Yonemori K, Tawada M, Sumi H, Satoh Y, Yamamoto Y, Miyahisa I, Sasaki M, Satomi Y, Hirayama M, Nishigaki R, Maezaki H. Imamura K, et al. Among authors: miyazaki t. Bioorg Med Chem. 2017 Jul 15;25(14):3768-3779. doi: 10.1016/j.bmc.2017.05.016. Epub 2017 May 11. Bioorg Med Chem. 2017. PMID: 28571972
4,204 results