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A covalent fragment-based strategy targeting a novel cysteine to inhibit activity of mutant EGFR kinase.
Kuki N, Walmsley DL, Kanai K, Takechi S, Yoshida M, Murakami R, Takano K, Tominaga Y, Takahashi M, Ito S, Nakao N, Angove H, Baker LM, Carter E, Dokurno P, Le Strat L, Macias AT, Molyneaux CA, Murray JB, Surgenor AE, Hamada T, Hubbard RE. Kuki N, et al. Among authors: takahashi m. RSC Med Chem. 2023 Oct 19;14(12):2731-2737. doi: 10.1039/d3md00439b. eCollection 2023 Dec 13. RSC Med Chem. 2023. PMID: 38107172
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: takahashi m. 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
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: takahashi m. 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
Identification of the 5,5-dioxo-7,8-dihydro-6H-thiopyrano[3,2-d]pyrimidine derivatives as highly selective PDE4B inhibitors.
Goto T, Shiina A, Murata T, Tomii M, Yamazaki T, Yoshida K, Yoshino T, Suzuki O, Sogawa Y, Mizukami K, Takagi N, Yoshitomi T, Etori M, Tsuchida H, Mikkaichi T, Nakao N, Takahashi M, Takahashi H, Sasaki S. Goto T, et al. Among authors: takahashi m, takahashi h. Bioorg Med Chem Lett. 2014 Feb 1;24(3):893-9. doi: 10.1016/j.bmcl.2013.12.076. Epub 2013 Dec 25. Bioorg Med Chem Lett. 2014. PMID: 24412069
Discovery of potent and orally active tricyclic-based FBPase inhibitors.
Tsukada T, Kanno O, Yamane T, Tanaka J, Yoshida T, Okuno A, Shiiki T, Takahashi M, Nishi T. Tsukada T, et al. Among authors: takahashi m. Bioorg Med Chem. 2010 Jul 15;18(14):5346-51. doi: 10.1016/j.bmc.2010.05.041. Epub 2010 May 20. Bioorg Med Chem. 2010. PMID: 20542703
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