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A selective inhibitor of PRMT5 with in vivo and in vitro potency in MCL models.
Chan-Penebre E, Kuplast KG, Majer CR, Boriack-Sjodin PA, Wigle TJ, Johnston LD, Rioux N, Munchhof MJ, Jin L, Jacques SL, West KA, Lingaraj T, Stickland K, Ribich SA, Raimondi A, Scott MP, Waters NJ, Pollock RM, Smith JJ, Barbash O, Pappalardi M, Ho TF, Nurse K, Oza KP, Gallagher KT, Kruger R, Moyer MP, Copeland RA, Chesworth R, Duncan KW. Chan-Penebre E, et al. Among authors: jacques sl. Nat Chem Biol. 2015 Jun;11(6):432-7. doi: 10.1038/nchembio.1810. Epub 2015 Apr 27. Nat Chem Biol. 2015. PMID: 25915199
Aryl Pyrazoles as Potent Inhibitors of Arginine Methyltransferases: Identification of the First PRMT6 Tool Compound.
Mitchell LH, Drew AE, Ribich SA, Rioux N, Swinger KK, Jacques SL, Lingaraj T, Boriack-Sjodin PA, Waters NJ, Wigle TJ, Moradei O, Jin L, Riera T, Porter-Scott M, Moyer MP, Smith JJ, Chesworth R, Copeland RA. Mitchell LH, et al. Among authors: jacques sl. ACS Med Chem Lett. 2015 Apr 6;6(6):655-9. doi: 10.1021/acsmedchemlett.5b00071. eCollection 2015 Jun 11. ACS Med Chem Lett. 2015. PMID: 26101569 Free PMC article.
Novel Oxindole Sulfonamides and Sulfamides: EPZ031686, the First Orally Bioavailable Small Molecule SMYD3 Inhibitor.
Mitchell LH, Boriack-Sjodin PA, Smith S, Thomenius M, Rioux N, Munchhof M, Mills JE, Klaus C, Totman J, Riera TV, Raimondi A, Jacques SL, West K, Foley M, Waters NJ, Kuntz KW, Wigle TJ, Scott MP, Copeland RA, Smith JJ, Chesworth R. Mitchell LH, et al. Among authors: jacques sl. ACS Med Chem Lett. 2015 Aug 27;7(2):134-8. doi: 10.1021/acsmedchemlett.5b00272. eCollection 2016 Feb 11. ACS Med Chem Lett. 2015. PMID: 26985287 Free PMC article.
Identification of a CARM1 Inhibitor with Potent In Vitro and In Vivo Activity in Preclinical Models of Multiple Myeloma.
Drew AE, Moradei O, Jacques SL, Rioux N, Boriack-Sjodin AP, Allain C, Scott MP, Jin L, Raimondi A, Handler JL, Ott HM, Kruger RG, McCabe MT, Sneeringer C, Riera T, Shapiro G, Waters NJ, Mitchell LH, Duncan KW, Moyer MP, Copeland RA, Smith J, Chesworth R, Ribich SA. Drew AE, et al. Among authors: jacques sl. Sci Rep. 2017 Dec 21;7(1):17993. doi: 10.1038/s41598-017-18446-z. Sci Rep. 2017. PMID: 29269946 Free PMC article.
Small molecule inhibitors and CRISPR/Cas9 mutagenesis demonstrate that SMYD2 and SMYD3 activity are dispensable for autonomous cancer cell proliferation.
Thomenius MJ, Totman J, Harvey D, Mitchell LH, Riera TV, Cosmopoulos K, Grassian AR, Klaus C, Foley M, Admirand EA, Jahic H, Majer C, Wigle T, Jacques SL, Gureasko J, Brach D, Lingaraj T, West K, Smith S, Rioux N, Waters NJ, Tang C, Raimondi A, Munchhof M, Mills JE, Ribich S, Porter Scott M, Kuntz KW, Janzen WP, Moyer M, Smith JJ, Chesworth R, Copeland RA, Boriack-Sjodin PA. Thomenius MJ, et al. Among authors: jacques sl. PLoS One. 2018 Jun 1;13(6):e0197372. doi: 10.1371/journal.pone.0197372. eCollection 2018. PLoS One. 2018. PMID: 29856759 Free PMC article.
Structure of the catalytic domain of human polo-like kinase 1.
Kothe M, Kohls D, Low S, Coli R, Cheng AC, Jacques SL, Johnson TL, Lewis C, Loh C, Nonomiya J, Sheils AL, Verdries KA, Wynn TA, Kuhn C, Ding YH. Kothe M, et al. Among authors: jacques sl. Biochemistry. 2007 May 22;46(20):5960-71. doi: 10.1021/bi602474j. Epub 2007 Apr 27. Biochemistry. 2007. PMID: 17461553
Enhanced selectivity profile of pyrazole-urea based DFG-out p38alpha inhibitors.
Liu H, Kuhn C, Feru F, Jacques SL, Deshmukh GD, Ye P, Rennie GR, Johnson T, Kazmirski S, Low S, Coli R, Ding YH, Cheng AC, Tecle H, English JM, Stanton R, Wu JC. Liu H, et al. Among authors: jacques sl. Bioorg Med Chem Lett. 2010 Aug 15;20(16):4885-91. doi: 10.1016/j.bmcl.2010.06.073. Epub 2010 Jun 17. Bioorg Med Chem Lett. 2010. PMID: 20620059
175 results