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A novel Menin-MLL1 inhibitor, DS-1594a, prevents the progression of acute leukemia with rearranged MLL1 or mutated NPM1.
Numata M, Haginoya N, Shiroishi M, Hirata T, Sato-Otsubo A, Yoshikawa K, Takata Y, Nagase R, Kashimoto Y, Suzuki M, Schulte N, Polier G, Kurimoto A, Tomoe Y, Toyota A, Yoneyama T, Imai E, Watanabe K, Hamada T, Kanada R, Watanabe J, Kagoshima Y, Tokumaru E, Murata K, Baba T, Shinozaki T, Ohtsuka M, Goto K, Karibe T, Deguchi T, Gocho Y, Yoshida M, Tomizawa D, Kato M, Tsutsumi S, Kitagawa M, Abe Y. Numata M, et al. Among authors: kanada r. Cancer Cell Int. 2023 Feb 25;23(1):36. doi: 10.1186/s12935-023-02877-y. Cancer Cell Int. 2023. PMID: 36841758 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. 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
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. 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