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Small-molecule inhibitors targeting Polycomb repressive complex 1 RING domain.
Shukla S, Ying W, Gray F, Yao Y, Simes ML, Zhao Q, Miao H, Cho HJ, González-Alonso P, Winkler A, Lund G, Purohit T, Kim E, Zhang X, Ray JM, He S, Nikolaidis C, Ndoj J, Wang J, Jaremko Ł, Jaremko M, Ryan RJH, Guzman ML, Grembecka J, Cierpicki T. Shukla S, et al. Nat Chem Biol. 2021 Jul;17(7):784-793. doi: 10.1038/s41589-021-00815-5. Epub 2021 Jun 21. Nat Chem Biol. 2021. PMID: 34155404 Free PMC article.
Development of potent dimeric inhibitors of GAS41 YEATS domain.
Listunov D, Linhares BM, Kim E, Winkler A, Simes ML, Weaver S, Cho HJ, Rizo A, Zolov S, Keshamouni VG, Grembecka J, Cierpicki T. Listunov D, et al. Cell Chem Biol. 2021 Dec 16;28(12):1716-1727.e6. doi: 10.1016/j.chembiol.2021.06.010. Epub 2021 Jul 21. Cell Chem Biol. 2021. PMID: 34289376 Free PMC article.
Discovery of first-in-class inhibitors of ASH1L histone methyltransferase with anti-leukemic activity.
Rogawski DS, Deng J, Li H, Miao H, Borkin D, Purohit T, Song J, Chase J, Li S, Ndoj J, Klossowski S, Kim E, Mao F, Zhou B, Ropa J, Krotoska MZ, Jin Z, Ernst P, Feng X, Huang G, Nishioka K, Kelly S, He M, Wen B, Sun D, Muntean A, Dou Y, Maillard I, Cierpicki T, Grembecka J. Rogawski DS, et al. Nat Commun. 2021 May 14;12(1):2792. doi: 10.1038/s41467-021-23152-6. Nat Commun. 2021. PMID: 33990599 Free PMC article.
Covalent inhibition of NSD1 histone methyltransferase.
Huang H, Howard CA, Zari S, Cho HJ, Shukla S, Li H, Ndoj J, González-Alonso P, Nikolaidis C, Abbott J, Rogawski DS, Potopnyk MA, Kempinska K, Miao H, Purohit T, Henderson A, Mapp A, Sulis ML, Ferrando A, Grembecka J, Cierpicki T. Huang H, et al. Nat Chem Biol. 2020 Dec;16(12):1403-1410. doi: 10.1038/s41589-020-0626-6. Epub 2020 Aug 31. Nat Chem Biol. 2020. PMID: 32868895 Free PMC article.