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Somatic mutations at EZH2 Y641 act dominantly through a mechanism of selectively altered PRC2 catalytic activity, to increase H3K27 trimethylation.
Yap DB, Chu J, Berg T, Schapira M, Cheng SW, Moradian A, Morin RD, Mungall AJ, Meissner B, Boyle M, Marquez VE, Marra MA, Gascoyne RD, Humphries RK, Arrowsmith CH, Morin GB, Aparicio SA. Yap DB, et al. Among authors: schapira m. Blood. 2011 Feb 24;117(8):2451-9. doi: 10.1182/blood-2010-11-321208. Epub 2010 Dec 29. Blood. 2011. PMID: 21190999 Free PMC article.
Structural genomics and drug discovery: all in the family.
Weigelt J, McBroom-Cerajewski LD, Schapira M, Zhao Y, Arrowsmith CH. Weigelt J, et al. Among authors: schapira m. Curr Opin Chem Biol. 2008 Feb;12(1):32-9. doi: 10.1016/j.cbpa.2008.01.045. Epub 2008 Mar 7. Curr Opin Chem Biol. 2008. PMID: 18282486 Review.
Human HDAC7 harbors a class IIa histone deacetylase-specific zinc binding motif and cryptic deacetylase activity.
Schuetz A, Min J, Allali-Hassani A, Schapira M, Shuen M, Loppnau P, Mazitschek R, Kwiatkowski NP, Lewis TA, Maglathin RL, McLean TH, Bochkarev A, Plotnikov AN, Vedadi M, Arrowsmith CH. Schuetz A, et al. Among authors: schapira m. J Biol Chem. 2008 Apr 25;283(17):11355-63. doi: 10.1074/jbc.M707362200. Epub 2008 Feb 19. J Biol Chem. 2008. PMID: 18285338 Free PMC article.
Methylation-state-specific recognition of histones by the MBT repeat protein L3MBTL2.
Guo Y, Nady N, Qi C, Allali-Hassani A, Zhu H, Pan P, Adams-Cioaba MA, Amaya MF, Dong A, Vedadi M, Schapira M, Read RJ, Arrowsmith CH, Min J. Guo Y, et al. Among authors: schapira m. Nucleic Acids Res. 2009 Apr;37(7):2204-10. doi: 10.1093/nar/gkp086. Epub 2009 Feb 20. Nucleic Acids Res. 2009. PMID: 19233876 Free PMC article.
Structural biology of human H3K9 methyltransferases.
Wu H, Min J, Lunin VV, Antoshenko T, Dombrovski L, Zeng H, Allali-Hassani A, Campagna-Slater V, Vedadi M, Arrowsmith CH, Plotnikov AN, Schapira M. Wu H, et al. Among authors: schapira m. PLoS One. 2010 Jan 11;5(1):e8570. doi: 10.1371/journal.pone.0008570. PLoS One. 2010. PMID: 20084102 Free PMC article.
Recognition and specificity determinants of the human cbx chromodomains.
Kaustov L, Ouyang H, Amaya M, Lemak A, Nady N, Duan S, Wasney GA, Li Z, Vedadi M, Schapira M, Min J, Arrowsmith CH. Kaustov L, et al. Among authors: schapira m. J Biol Chem. 2011 Jan 7;286(1):521-9. doi: 10.1074/jbc.M110.191411. Epub 2010 Nov 3. J Biol Chem. 2011. PMID: 21047797 Free PMC article.
Epigenetic protein families: a new frontier for drug discovery.
Arrowsmith CH, Bountra C, Fish PV, Lee K, Schapira M. Arrowsmith CH, et al. Among authors: schapira m. Nat Rev Drug Discov. 2012 Apr 13;11(5):384-400. doi: 10.1038/nrd3674. Nat Rev Drug Discov. 2012. PMID: 22498752 Review.
Small-molecule inhibition of MLL activity by disruption of its interaction with WDR5.
Senisterra G, Wu H, Allali-Hassani A, Wasney GA, Barsyte-Lovejoy D, Dombrovski L, Dong A, Nguyen KT, Smil D, Bolshan Y, Hajian T, He H, Seitova A, Chau I, Li F, Poda G, Couture JF, Brown PJ, Al-Awar R, Schapira M, Arrowsmith CH, Vedadi M. Senisterra G, et al. Among authors: schapira m. Biochem J. 2013 Jan 1;449(1):151-9. doi: 10.1042/BJ20121280. Biochem J. 2013. PMID: 22989411 Free PMC article.
Catalytic site remodelling of the DOT1L methyltransferase by selective inhibitors.
Yu W, Chory EJ, Wernimont AK, Tempel W, Scopton A, Federation A, Marineau JJ, Qi J, Barsyte-Lovejoy D, Yi J, Marcellus R, Iacob RE, Engen JR, Griffin C, Aman A, Wienholds E, Li F, Pineda J, Estiu G, Shatseva T, Hajian T, Al-Awar R, Dick JE, Vedadi M, Brown PJ, Arrowsmith CH, Bradner JE, Schapira M. Yu W, et al. Among authors: schapira m. Nat Commun. 2012;3:1288. doi: 10.1038/ncomms2304. Nat Commun. 2012. PMID: 23250418 Free article.
548 results