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Page 1
Discovery of novel histone lysine methyltransferase G9a/GLP (EHMT2/1) inhibitors: Design, synthesis, and structure-activity relationships of 2,4-diamino-6-methylpyrimidines.
Katayama K, Ishii K, Tsuda E, Yotsumoto K, Hiramoto K, Suzuki M, Yasumatsu I, Igarashi W, Torihata M, Ishiyama T, Katagiri T. Katayama K, et al. Among authors: yasumatsu i. Bioorg Med Chem Lett. 2020 Oct 15;30(20):127475. doi: 10.1016/j.bmcl.2020.127475. Epub 2020 Aug 8. Bioorg Med Chem Lett. 2020. PMID: 32781218
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: yasumatsu i. 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.
Novel orally bioavailable EZH1/2 dual inhibitors with greater antitumor efficacy than an EZH2 selective inhibitor.
Honma D, Kanno O, Watanabe J, Kinoshita J, Hirasawa M, Nosaka E, Shiroishi M, Takizawa T, Yasumatsu I, Horiuchi T, Nakao A, Suzuki K, Yamasaki T, Nakajima K, Hayakawa M, Yamazaki T, Yadav AS, Adachi N. Honma D, et al. Among authors: yasumatsu i. Cancer Sci. 2017 Oct;108(10):2069-2078. doi: 10.1111/cas.13326. Epub 2017 Aug 8. Cancer Sci. 2017. PMID: 28741798 Free PMC article.
Discovery of Novel Pyrido-pyridazinone Derivatives as FER Tyrosine Kinase Inhibitors with Antitumor Activity.
Taniguchi T, Inagaki H, Baba D, Yasumatsu I, Toyota A, Kaneta Y, Kiga M, Iimura S, Odagiri T, Shibata Y, Ueda K, Seo M, Shimizu H, Imaoka T, Nakayama K. Taniguchi T, et al. Among authors: yasumatsu i. ACS Med Chem Lett. 2019 Mar 15;10(5):737-742. doi: 10.1021/acsmedchemlett.8b00631. eCollection 2019 May 9. ACS Med Chem Lett. 2019. PMID: 31097992 Free PMC article.
Discovery of DS79932728: A Potent, Orally Available G9a/GLP Inhibitor for Treating β-Thalassemia and Sickle Cell Disease.
Katayama K, Ishii K, Terashima H, Tsuda E, Suzuki M, Yotsumoto K, Hiramoto K, Yasumatsu I, Torihata M, Ishiyama T, Muto T, Katagiri T. Katayama K, et al. Among authors: yasumatsu i. ACS Med Chem Lett. 2020 Dec 28;12(1):121-128. doi: 10.1021/acsmedchemlett.0c00572. eCollection 2021 Jan 14. ACS Med Chem Lett. 2020. PMID: 33488973 Free PMC article.
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