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A non-canonical SWI/SNF complex is a synthetic lethal target in cancers driven by BAF complex perturbation.
Michel BC, D'Avino AR, Cassel SH, Mashtalir N, McKenzie ZM, McBride MJ, Valencia AM, Zhou Q, Bocker M, Soares LMM, Pan J, Remillard DI, Lareau CA, Zullow HJ, Fortoul N, Gray NS, Bradner JE, Chan HM, Kadoch C. Michel BC, et al. Among authors: chan hm. Nat Cell Biol. 2018 Dec;20(12):1410-1420. doi: 10.1038/s41556-018-0221-1. Epub 2018 Nov 5. Nat Cell Biol. 2018. PMID: 30397315 Free PMC article.
An allosteric PRC2 inhibitor targeting the H3K27me3 binding pocket of EED.
Qi W, Zhao K, Gu J, Huang Y, Wang Y, Zhang H, Zhang M, Zhang J, Yu Z, Li L, Teng L, Chuai S, Zhang C, Zhao M, Chan H, Chen Z, Fang D, Fei Q, Feng L, Feng L, Gao Y, Ge H, Ge X, Li G, Lingel A, Lin Y, Liu Y, Luo F, Shi M, Wang L, Wang Z, Yu Y, Zeng J, Zeng C, Zhang L, Zhang Q, Zhou S, Oyang C, Atadja P, Li E. Qi W, et al. Nat Chem Biol. 2017 Apr;13(4):381-388. doi: 10.1038/nchembio.2304. Epub 2017 Jan 30. Nat Chem Biol. 2017. PMID: 28135235
Selective inhibition of Ezh2 by a small molecule inhibitor blocks tumor cells proliferation.
Qi W, Chan H, Teng L, Li L, Chuai S, Zhang R, Zeng J, Li M, Fan H, Lin Y, Gu J, Ardayfio O, Zhang JH, Yan X, Fang J, Mi Y, Zhang M, Zhou T, Feng G, Chen Z, Li G, Yang T, Zhao K, Liu X, Yu Z, Lu CX, Atadja P, Li E. Qi W, et al. Proc Natl Acad Sci U S A. 2012 Dec 26;109(52):21360-5. doi: 10.1073/pnas.1210371110. Epub 2012 Dec 10. Proc Natl Acad Sci U S A. 2012. PMID: 23236167 Free PMC article.
Histone methylation by PRC2 is inhibited by active chromatin marks.
Schmitges FW, Prusty AB, Faty M, Stützer A, Lingaraju GM, Aiwazian J, Sack R, Hess D, Li L, Zhou S, Bunker RD, Wirth U, Bouwmeester T, Bauer A, Ly-Hartig N, Zhao K, Chan H, Gu J, Gut H, Fischle W, Müller J, Thomä NH. Schmitges FW, et al. Mol Cell. 2011 May 6;42(3):330-41. doi: 10.1016/j.molcel.2011.03.025. Mol Cell. 2011. PMID: 21549310 Free article.
NSD2 is recruited through its PHD domain to oncogenic gene loci to drive multiple myeloma.
Huang Z, Wu H, Chuai S, Xu F, Yan F, Englund N, Wang Z, Zhang H, Fang M, Wang Y, Gu J, Zhang M, Yang T, Zhao K, Yu Y, Dai J, Yi W, Zhou S, Li Q, Wu J, Liu J, Wu X, Chan H, Lu C, Atadja P, Li E, Wang Y, Hu M. Huang Z, et al. Cancer Res. 2013 Oct 15;73(20):6277-88. doi: 10.1158/0008-5472.CAN-13-1000. Epub 2013 Aug 26. Cancer Res. 2013. PMID: 23980095
419 results