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Discovery of DS-9300: A Highly Potent, Selective, and Once-Daily Oral EP300/CBP Histone Acetyltransferase Inhibitor.
Kanada R, Kagoshima Y, Suzuki T, Nakamura A, Funami H, Watanabe J, Asano M, Takahashi M, Ubukata O, Suzuki K, Aikawa T, Sato K, Goto M, Setsu G, Ito K, Kihara K, Kuroha M, Kohno T, Ogiwara H, Isoyama T, Tominaga Y, Higuchi S, Naito H. Kanada R, et al. Among authors: ubukata o. J Med Chem. 2023 Jan 12;66(1):695-715. doi: 10.1021/acs.jmedchem.2c01641. Epub 2022 Dec 26. J Med Chem. 2023. PMID: 36572866
A novel inhibitor stabilizes the inactive conformation of MAPK-interacting kinase 1.
Matsui Y, Yasumatsu I, Yoshida KI, Iimura S, Ikeno Y, Nawano T, Fukano H, Ubukata O, Hanzawa H, Tanzawa F, Isoyama T. Matsui Y, et al. Among authors: ubukata o. Acta Crystallogr F Struct Biol Commun. 2018 Mar 1;74(Pt 3):156-160. doi: 10.1107/S2053230X18002108. Epub 2018 Feb 26. Acta Crystallogr F Struct Biol Commun. 2018. PMID: 29497019 Free PMC article.
Discovery of EP300/CBP histone acetyltransferase inhibitors through scaffold hopping of 1,4-oxazepane ring.
Kanada R, Kagoshima Y, Asano M, Suzuki T, Murata T, Haruta M, Takahashi M, Ubukata O, Hashimoto K, Obata K, Kihara K, Kuroha M, Banjo T, Togashi N, Sato K, Yamamoto Y, Suzuki K, Isoyama T, Tominaga Y, Higuchi S, Naito H. Kanada R, et al. Among authors: ubukata o. Bioorg Med Chem Lett. 2022 Jun 15;66:128726. doi: 10.1016/j.bmcl.2022.128726. Epub 2022 Apr 9. Bioorg Med Chem Lett. 2022. PMID: 35413416
Novel protein kinase cAMP-Activated Catalytic Subunit Alpha (PRKACA) inhibitor shows anti-tumor activity in a fibrolamellar hepatocellular carcinoma model.
Toyota A, Goto M, Miyamoto M, Nagashima Y, Iwasaki S, Komatsu T, Momose T, Yoshida K, Tsukada T, Matsufuji T, Ohno A, Suzuki M, Ubukata O, Kaneta Y. Toyota A, et al. Among authors: ubukata o. Biochem Biophys Res Commun. 2022 Sep 17;621:157-161. doi: 10.1016/j.bbrc.2022.07.008. Epub 2022 Jul 7. Biochem Biophys Res Commun. 2022. PMID: 35839742
Discovery of a Novel ATP-Competitive MEK Inhibitor DS03090629 that Overcomes Resistance Conferred by BRAF Overexpression in BRAF-Mutated Melanoma.
Takano K, Munehira Y, Hatanaka M, Murakami R, Shibata Y, Shida T, Takeuchi K, Takechi S, Tabata T, Shimada T, Kishikawa S, Matsui Y, Ubukata O, Seki T, Kaneta Y. Takano K, et al. Among authors: ubukata o. Mol Cancer Ther. 2023 Mar 2;22(3):317-332. doi: 10.1158/1535-7163.MCT-22-0306. Mol Cancer Ther. 2023. PMID: 36622773
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