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Page 1
Target 2035 - update on the quest for a probe for every protein.
Müller S, Ackloo S, Al Chawaf A, Al-Lazikani B, Antolin A, Baell JB, Beck H, Beedie S, Betz UAK, Bezerra GA, Brennan PE, Brown D, Brown PJ, Bullock AN, Carter AJ, Chaikuad A, Chaineau M, Ciulli A, Collins I, Dreher J, Drewry D, Edfeldt K, Edwards AM, Egner U, Frye SV, Fuchs SM, Hall MD, Hartung IV, Hillisch A, Hitchcock SH, Homan E, Kannan N, Kiefer JR, Knapp S, Kostic M, Kubicek S, Leach AR, Lindemann S, Marsden BD, Matsui H, Meier JL, Merk D, Michel M, Morgan MR, Mueller-Fahrnow A, Owen DR, Perry BG, Rosenberg SH, Saikatendu KS, Schapira M, Scholten C, Sharma S, Simeonov A, Sundström M, Superti-Furga G, Todd MH, Tredup C, Vedadi M, von Delft F, Willson TM, Winter GE, Workman P, Arrowsmith CH. Müller S, et al. Among authors: frye sv. RSC Med Chem. 2021 Dec 3;13(1):13-21. doi: 10.1039/d1md00228g. eCollection 2022 Jan 27. RSC Med Chem. 2021. PMID: 35211674 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.
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.
Too many roads not taken.
Edwards AM, Isserlin R, Bader GD, Frye SV, Willson TM, Yu FH. Edwards AM, et al. Among authors: frye sv. Nature. 2011 Feb 10;470(7333):163-5. doi: 10.1038/470163a. Nature. 2011. PMID: 21307913 No abstract available.
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.
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: frye sv. 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.
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: frye sv. 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.
148 results