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Discovery of 3-Ethyl-4-(3-isopropyl-4-(4-(1-methyl-1 H-pyrazol-4-yl)-1 H-imidazol-1-yl)-1 H-pyrazolo[3,4- b]pyridin-1-yl)benzamide (TAS-116) as a Potent, Selective, and Orally Available HSP90 Inhibitor.
Uno T, Kawai Y, Yamashita S, Oshiumi H, Yoshimura C, Mizutani T, Suzuki T, Chong KT, Shigeno K, Ohkubo M, Kodama Y, Muraoka H, Funabashi K, Takahashi K, Ohkubo S, Kitade M. Uno T, et al. Among authors: ohkubo s, ohkubo m. J Med Chem. 2019 Jan 24;62(2):531-551. doi: 10.1021/acs.jmedchem.8b01085. Epub 2018 Dec 21. J Med Chem. 2019. PMID: 30525599
First-in-Human Phase I Study of an Oral HSP90 Inhibitor, TAS-116, in Patients with Advanced Solid Tumors.
Shimomura A, Yamamoto N, Kondo S, Fujiwara Y, Suzuki S, Yanagitani N, Horiike A, Kitazono S, Ohyanagi F, Doi T, Kuboki Y, Kawazoe A, Shitara K, Ohno I, Banerji U, Sundar R, Ohkubo S, Calleja EM, Nishio M. Shimomura A, et al. Among authors: ohkubo s. Mol Cancer Ther. 2019 Mar;18(3):531-540. doi: 10.1158/1535-7163.MCT-18-0831. Epub 2019 Jan 24. Mol Cancer Ther. 2019. PMID: 30679388 Clinical Trial.
TAS4464, A Highly Potent and Selective Inhibitor of NEDD8-Activating Enzyme, Suppresses Neddylation and Shows Antitumor Activity in Diverse Cancer Models.
Yoshimura C, Muraoka H, Ochiiwa H, Tsuji S, Hashimoto A, Kazuno H, Nakagawa F, Komiya Y, Suzuki S, Takenaka T, Kumazaki M, Fujita N, Mizutani T, Ohkubo S. Yoshimura C, et al. Among authors: ohkubo s. Mol Cancer Ther. 2019 Jul;18(7):1205-1216. doi: 10.1158/1535-7163.MCT-18-0644. Epub 2019 May 15. Mol Cancer Ther. 2019. PMID: 31092565
TAS4464, a NEDD8-activating enzyme inhibitor, activates both intrinsic and extrinsic apoptotic pathways via c-Myc-mediated regulation in acute myeloid leukemia.
Ochiiwa H, Ailiken G, Yokoyama M, Yamagata K, Nagano H, Yoshimura C, Muraoka H, Ishida K, Haruma T, Nakayama A, Hashimoto N, Murata K, Nishimura M, Kawashima Y, Ohara O, Ohkubo S, Tanaka T. Ochiiwa H, et al. Among authors: ohkubo s. Oncogene. 2021 Feb;40(7):1217-1230. doi: 10.1038/s41388-020-01586-4. Epub 2021 Jan 8. Oncogene. 2021. PMID: 33420360 Free PMC article.
Thermodynamic Dissection of Potency and Selectivity of Cytosolic Hsp90 Inhibitors.
Yoshimura C, Nagatoishi S, Kuroda D, Kodama Y, Uno T, Kitade M, Chong-Takata K, Oshiumi H, Muraoka H, Yamashita S, Kawai Y, Ohkubo S, Tsumoto K. Yoshimura C, et al. Among authors: ohkubo s. J Med Chem. 2021 Mar 11;64(5):2669-2677. doi: 10.1021/acs.jmedchem.0c01715. Epub 2021 Feb 23. J Med Chem. 2021. PMID: 33621080 Free article.
Vepafestinib is a pharmacologically advanced RET-selective inhibitor with high CNS penetration and inhibitory activity against RET solvent front mutations.
Miyazaki I, Odintsov I, Ishida K, Lui AJW, Kato M, Suzuki T, Zhang T, Wakayama K, Kurth RI, Cheng R, Fujita H, Delasos L, Vojnic M, Khodos I, Yamada Y, Ishizawa K, Mattar MS, Funabashi K, Chang Q, Ohkubo S, Yano W, Terada R, Giuliano C, Lu YC, Bonifacio A, Kunte S, Davare MA, Cheng EH, de Stanchina E, Lovati E, Iwasawa Y, Ladanyi M, Somwar R. Miyazaki I, et al. Among authors: ohkubo s. Nat Cancer. 2023 Sep;4(9):1345-1361. doi: 10.1038/s43018-023-00630-y. Epub 2023 Sep 21. Nat Cancer. 2023. PMID: 37743366 Free PMC article.
290 results