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A potent, selective and cell-active allosteric inhibitor of protein arginine methyltransferase 3 (PRMT3).
Kaniskan HÜ, Szewczyk MM, Yu Z, Eram MS, Yang X, Schmidt K, Luo X, Dai M, He F, Zang I, Lin Y, Kennedy S, Li F, Dobrovetsky E, Dong A, Smil D, Min SJ, Landon M, Lin-Jones J, Huang XP, Roth BL, Schapira M, Atadja P, Barsyte-Lovejoy D, Arrowsmith CH, Brown PJ, Zhao K, Jin J, Vedadi M. Kaniskan HÜ, et al. Among authors: roth bl. Angew Chem Int Ed Engl. 2015 Apr 20;54(17):5166-70. doi: 10.1002/anie.201412154. Epub 2015 Feb 27. Angew Chem Int Ed Engl. 2015. PMID: 25728001 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: roth bl. Nat Chem Biol. 2011 Jul 10;7(8):566-74. doi: 10.1038/nchembio.599. Nat Chem Biol. 2011. PMID: 21743462 Free PMC article.
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: roth bl. 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 an in vivo chemical probe of the lysine methyltransferases G9a and GLP.
Liu F, Barsyte-Lovejoy D, Li F, Xiong Y, Korboukh V, Huang XP, Allali-Hassani A, Janzen WP, Roth BL, Frye SV, Arrowsmith CH, Brown PJ, Vedadi M, Jin J. Liu F, et al. Among authors: roth bl. J Med Chem. 2013 Nov 14;56(21):8931-42. doi: 10.1021/jm401480r. Epub 2013 Oct 31. J Med Chem. 2013. PMID: 24102134 Free PMC article.
Identification of novel functionally selective κ-opioid receptor scaffolds.
White KL, Scopton AP, Rives ML, Bikbulatov RV, Polepally PR, Brown PJ, Kenakin T, Javitch JA, Zjawiony JK, Roth BL. White KL, et al. Among authors: roth bl. Mol Pharmacol. 2014 Jan;85(1):83-90. doi: 10.1124/mol.113.089649. Epub 2013 Oct 10. Mol Pharmacol. 2014. PMID: 24113749 Free PMC article.
Molecular control of δ-opioid receptor signalling.
Fenalti G, Giguere PM, Katritch V, Huang XP, Thompson AA, Cherezov V, Roth BL, Stevens RC. Fenalti G, et al. Among authors: roth bl. Nature. 2014 Feb 13;506(7487):191-6. doi: 10.1038/nature12944. Epub 2014 Jan 12. Nature. 2014. PMID: 24413399 Free PMC article.
Allosteric ligands for the pharmacologically dark receptors GPR68 and GPR65.
Huang XP, Karpiak J, Kroeze WK, Zhu H, Chen X, Moy SS, Saddoris KA, Nikolova VD, Farrell MS, Wang S, Mangano TJ, Deshpande DA, Jiang A, Penn RB, Jin J, Koller BH, Kenakin T, Shoichet BK, Roth BL. Huang XP, et al. Among authors: roth bl. Nature. 2015 Nov 26;527(7579):477-83. doi: 10.1038/nature15699. Epub 2015 Nov 9. Nature. 2015. PMID: 26550826 Free PMC article.
538 results