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An orally bioavailable chemical probe of the Lysine Methyltransferases EZH2 and EZH1.
Konze KD, Ma A, Li F, Barsyte-Lovejoy D, Parton T, Macnevin CJ, Liu F, Gao C, Huang XP, Kuznetsova E, Rougie M, Jiang A, Pattenden SG, Norris JL, James LI, Roth BL, Brown PJ, Frye SV, Arrowsmith CH, Hahn KM, Wang GG, Vedadi M, Jin J. Konze KD, et al. Among authors: frye sv. ACS Chem Biol. 2013;8(6):1324-34. doi: 10.1021/cb400133j. Epub 2013 Apr 24. ACS Chem Biol. 2013. PMID: 23614352 Free PMC 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: frye sv. J Med Chem. 2009 Dec 24;52(24):7950-3. doi: 10.1021/jm901543m. J Med Chem. 2009. PMID: 19891491 Free PMC article.
The art of the chemical probe.
Frye SV. Frye SV. Nat Chem Biol. 2010 Mar;6(3):159-161. doi: 10.1038/nchembio.296. Nat Chem Biol. 2010. PMID: 20154659 No abstract available.
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: frye sv. J Med Chem. 2010 Aug 12;53(15):5844-57. doi: 10.1021/jm100478y. J Med Chem. 2010. PMID: 20614940 Free PMC article.
Epigenetics: Tools and Technologies.
Janzen WP, Wigle TJ, Jin J, Frye SV. Janzen WP, et al. Among authors: frye sv. Drug Discov Today Technol. 2010 Spring;7(1):e59-e65. doi: 10.1016/j.ddtec.2010.07.004. Drug Discov Today Technol. 2010. PMID: 21243036 Free PMC article.
Small-molecule ligands of methyl-lysine binding proteins.
Herold JM, Wigle TJ, Norris JL, Lam R, Korboukh VK, Gao C, Ingerman LA, Kireev DB, Senisterra G, Vedadi M, Tripathy A, Brown PJ, Arrowsmith CH, Jin J, Janzen WP, Frye SV. Herold JM, et al. Among authors: frye sv. J Med Chem. 2011 Apr 14;54(7):2504-11. doi: 10.1021/jm200045v. Epub 2011 Mar 18. J Med Chem. 2011. PMID: 21417280 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: frye sv. Nat Chem Biol. 2011 Jul 10;7(8):566-74. doi: 10.1038/nchembio.599. Nat Chem Biol. 2011. PMID: 21743462 Free PMC article.
148 results