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Discovery of Potent and Selective Allosteric Inhibitors of Protein Arginine Methyltransferase 3 (PRMT3).
Kaniskan HÜ, Eram MS, Zhao K, Szewczyk MM, Yang X, Schmidt K, Luo X, Xiao S, Dai M, He F, Zang I, Lin Y, Li F, Dobrovetsky E, Smil D, Min SJ, Lin-Jones J, Schapira M, Atadja P, Li E, Barsyte-Lovejoy D, Arrowsmith CH, Brown PJ, Liu F, Yu Z, Vedadi M, Jin J. Kaniskan HÜ, et al. Among authors: li e, li f. J Med Chem. 2018 Feb 8;61(3):1204-1217. doi: 10.1021/acs.jmedchem.7b01674. Epub 2018 Jan 5. J Med Chem. 2018. PMID: 29244490 Free PMC article.
Structure-activity relationship studies of G9a-like protein (GLP) inhibitors.
Xiong Y, Li F, Babault N, Wu H, Dong A, Zeng H, Chen X, Arrowsmith CH, Brown PJ, Liu J, Vedadi M, Jin J. Xiong Y, et al. Among authors: li f. Bioorg Med Chem. 2017 Aug 15;25(16):4414-4423. doi: 10.1016/j.bmc.2017.06.021. Epub 2017 Jun 19. Bioorg Med Chem. 2017. PMID: 28662962 Free PMC article.
LLY-283, a Potent and Selective Inhibitor of Arginine Methyltransferase 5, PRMT5, with Antitumor Activity.
Bonday ZQ, Cortez GS, Grogan MJ, Antonysamy S, Weichert K, Bocchinfuso WP, Li F, Kennedy S, Li B, Mader MM, Arrowsmith CH, Brown PJ, Eram MS, Szewczyk MM, Barsyte-Lovejoy D, Vedadi M, Guccione E, Campbell RM. Bonday ZQ, et al. Among authors: li f, li b. ACS Med Chem Lett. 2018 Apr 23;9(7):612-617. doi: 10.1021/acsmedchemlett.8b00014. eCollection 2018 Jul 12. ACS Med Chem Lett. 2018. PMID: 30034588 Free PMC article.
Discovery of a Potent and Selective Fragment-like Inhibitor of Methyllysine Reader Protein Spindlin 1 (SPIN1).
Xiong Y, Greschik H, Johansson C, Seifert L, Bacher J, Park KS, Babault N, Martini M, Fagan V, Li F, Chau I, Christott T, Dilworth D, Barsyte-Lovejoy D, Vedadi M, Arrowsmith CH, Brennan P, Fedorov O, Jung M, Farnie G, Liu J, Oppermann U, Schüle R, Jin J. Xiong Y, et al. Among authors: li f. J Med Chem. 2019 Oct 24;62(20):8996-9007. doi: 10.1021/acs.jmedchem.9b00522. Epub 2019 Jul 24. J Med Chem. 2019. PMID: 31260300
Selective, Small-Molecule Co-Factor Binding Site Inhibition of a Su(var)3-9, Enhancer of Zeste, Trithorax Domain Containing Lysine Methyltransferase.
Taylor AP, Swewczyk M, Kennedy S, Trush VV, Wu H, Zeng H, Dong A, Ferreira de Freitas R, Tatlock J, Kumpf RA, Wythes M, Casimiro-Garcia A, Denny RA, Parikh MD, Li F, Barsyte-Lovejoy D, Schapira M, Vedadi M, Brown PJ, Arrowsmith CH, Owen DR. Taylor AP, et al. Among authors: li f. J Med Chem. 2019 Sep 12;62(17):7669-7683. doi: 10.1021/acs.jmedchem.9b00112. Epub 2019 Sep 3. J Med Chem. 2019. PMID: 31415173
Chemical probes for protein arginine methyltransferases.
Li ASM, Li F, Eram MS, Bolotokova A, Dela Seña CC, Vedadi M. Li ASM, et al. Among authors: li f. Methods. 2020 Mar 15;175:30-43. doi: 10.1016/j.ymeth.2019.11.017. Epub 2019 Dec 3. Methods. 2020. PMID: 31809836 Review.
Discovery of Small-Molecule Antagonists of the PWWP Domain of NSD2.
Ferreira de Freitas R, Liu Y, Szewczyk MM, Mehta N, Li F, McLeod D, Zepeda-Velázquez C, Dilworth D, Hanley RP, Gibson E, Brown PJ, Al-Awar R, James LI, Arrowsmith CH, Barsyte-Lovejoy D, Min J, Vedadi M, Schapira M, Allali-Hassani A. Ferreira de Freitas R, et al. Among authors: li f. J Med Chem. 2021 Feb 11;64(3):1584-1592. doi: 10.1021/acs.jmedchem.0c01768. Epub 2021 Feb 1. J Med Chem. 2021. PMID: 33522809 Free PMC article.
A First-in-Class, Highly Selective and Cell-Active Allosteric Inhibitor of Protein Arginine Methyltransferase 6.
Shen Y, Li F, Szewczyk MM, Halabelian L, Chau I, Eram MS, Dela Seña C, Park KS, Meng F, Chen H, Zeng H, Dong A, Wu H, Trush VV, McLeod D, Zepeda-Velázquez CA, Campbell RM, Mader MM, Watson BM, Schapira M, Arrowsmith CH, Al-Awar R, Barsyte-Lovejoy D, Kaniskan HÜ, Brown PJ, Vedadi M, Jin J. Shen Y, et al. Among authors: li f. J Med Chem. 2021 Apr 8;64(7):3697-3706. doi: 10.1021/acs.jmedchem.0c02160. Epub 2021 Feb 16. J Med Chem. 2021. PMID: 33591753 Free PMC article.
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