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Page 1
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: brown pj. Nat Commun. 2012;3:1288. doi: 10.1038/ncomms2304. Nat Commun. 2012. PMID: 23250418 Free article.
Discovery of a 2,4-diamino-7-aminoalkoxyquinazoline as a potent and selective inhibitor of histone lysine methyltransferase G9a.
Liu F, Chen X, Allali-Hassani A, Quinn AM, Wasney GA, Dong A, Barsyte D, Kozieradzki I, Senisterra G, Chau I, Siarheyeva A, Kireev DB, Jadhav A, Herold JM, Frye SV, Arrowsmith CH, Brown PJ, Simeonov A, Vedadi M, Jin J. Liu F, et al. Among authors: brown pj. J Med Chem. 2009 Dec 24;52(24):7950-3. doi: 10.1021/jm901543m. J Med Chem. 2009. PMID: 19891491 Free PMC article.
Protein lysine methyltransferase G9a inhibitors: design, synthesis, and structure activity relationships of 2,4-diamino-7-aminoalkoxy-quinazolines.
Liu F, Chen X, Allali-Hassani A, Quinn AM, Wigle TJ, Wasney GA, Dong A, Senisterra G, Chau I, Siarheyeva A, Norris JL, Kireev DB, Jadhav A, Herold JM, Janzen WP, Arrowsmith CH, Frye SV, Brown PJ, Simeonov A, Vedadi M, Jin J. Liu F, et al. Among authors: brown pj. J Med Chem. 2010 Aug 12;53(15):5844-57. doi: 10.1021/jm100478y. J Med Chem. 2010. PMID: 20614940 Free PMC article.
A chemical probe selectively inhibits G9a and GLP methyltransferase activity in cells.
Vedadi M, Barsyte-Lovejoy D, Liu F, Rival-Gervier S, Allali-Hassani A, Labrie V, Wigle TJ, Dimaggio PA, Wasney GA, Siarheyeva A, Dong A, Tempel W, Wang SC, Chen X, Chau I, Mangano TJ, Huang XP, Simpson CD, Pattenden SG, Norris JL, Kireev DB, Tripathy A, Edwards A, Roth BL, Janzen WP, Garcia BA, Petronis A, Ellis J, Brown PJ, Frye SV, Arrowsmith CH, Jin J. Vedadi M, et al. Among authors: brown pj. Nat Chem Biol. 2011 Jul 10;7(8):566-74. doi: 10.1038/nchembio.599. Nat Chem Biol. 2011. PMID: 21743462 Free PMC article.
Optimization of cellular activity of G9a inhibitors 7-aminoalkoxy-quinazolines.
Liu F, Barsyte-Lovejoy D, Allali-Hassani A, He Y, Herold JM, Chen X, Yates CM, Frye SV, Brown PJ, Huang J, Vedadi M, Arrowsmith CH, Jin J. Liu F, et al. Among authors: brown pj. J Med Chem. 2011 Sep 8;54(17):6139-50. doi: 10.1021/jm200903z. Epub 2011 Aug 5. J Med Chem. 2011. PMID: 21780790 Free PMC article.
An allosteric inhibitor of protein arginine methyltransferase 3.
Siarheyeva A, Senisterra G, Allali-Hassani A, Dong A, Dobrovetsky E, Wasney GA, Chau I, Marcellus R, Hajian T, Liu F, Korboukh I, Smil D, Bolshan Y, Min J, Wu H, Zeng H, Loppnau P, Poda G, Griffin C, Aman A, Brown PJ, Jin J, Al-Awar R, Arrowsmith CH, Schapira M, Vedadi M. Siarheyeva A, et al. Among authors: brown pj. Structure. 2012 Aug 8;20(8):1425-35. doi: 10.1016/j.str.2012.06.001. Epub 2012 Jul 12. Structure. 2012. PMID: 22795084 Free article.
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: brown pj. Biochem J. 2013 Jan 1;449(1):151-9. doi: 10.1042/BJ20121280. Biochem J. 2013. PMID: 22989411 Free PMC article.
Discovery of a chemical probe for the L3MBTL3 methyllysine reader domain.
James LI, Barsyte-Lovejoy D, Zhong N, Krichevsky L, Korboukh VK, Herold JM, MacNevin CJ, Norris JL, Sagum CA, Tempel W, Marcon E, Guo H, Gao C, Huang XP, Duan S, Emili A, Greenblatt JF, Kireev DB, Jin J, Janzen WP, Brown PJ, Bedford MT, Arrowsmith CH, Frye SV. James LI, et al. Among authors: brown pj. Nat Chem Biol. 2013 Mar;9(3):184-91. doi: 10.1038/nchembio.1157. Epub 2013 Jan 6. Nat Chem Biol. 2013. PMID: 23292653 Free PMC article.
679 results