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GNE-064: A Potent, Selective, and Orally Bioavailable Chemical Probe for the Bromodomains of SMARCA2 and SMARCA4 and the Fifth Bromodomain of PBRM1.
Taylor AM, Bailey C, Belmont LD, Campbell R, Cantone N, Côté A, Crawford TD, Cummings R, DeMent K, Duplessis M, Flynn M, Good AC, Huang HR, Joshi S, Leblanc Y, Murray J, Nasveschuk CG, Neiss A, Poy F, Romero FA, Sandy P, Tang Y, Tsui V, Zawadzke L, Sims RJ 3rd, Audia JE, Bellon SF, Magnuson SR, Albrecht BK, Cochran AG. Taylor AM, et al. Among authors: sims rj 3rd. J Med Chem. 2022 Aug 25;65(16):11177-11186. doi: 10.1021/acs.jmedchem.2c00662. Epub 2022 Aug 5. J Med Chem. 2022. PMID: 35930799
Identification and characterization of second-generation EZH2 inhibitors with extended residence times and improved biological activity.
Stuckey JI, Cantone NR, Côté A, Arora S, Vivat V, Ramakrishnan A, Mertz JA, Khanna A, Brenneman J, Gehling VS, Moine L, Sims RJ 3rd, Audia JE, Trojer P, Levell JR, Cummings RT. Stuckey JI, et al. Among authors: sims rj 3rd. J Biol Chem. 2021 Jan-Jun;296:100349. doi: 10.1016/j.jbc.2021.100349. Epub 2021 Jan 30. J Biol Chem. 2021. PMID: 33524394 Free PMC article.
Discovery of CPI-1612: A Potent, Selective, and Orally Bioavailable EP300/CBP Histone Acetyltransferase Inhibitor.
Wilson JE, Patel G, Patel C, Brucelle F, Huhn A, Gardberg AS, Poy F, Cantone N, Bommi-Reddy A, Sims RJ 3rd, Cummings RT, Levell JR. Wilson JE, et al. Among authors: sims rj 3rd. ACS Med Chem Lett. 2020 Apr 23;11(6):1324-1329. doi: 10.1021/acsmedchemlett.0c00155. eCollection 2020 Jun 11. ACS Med Chem Lett. 2020. PMID: 32551019 Free PMC article.
Design, Synthesis, and Pharmacological Evaluation of Second Generation EZH2 Inhibitors with Long Residence Time.
Khanna A, Côté A, Arora S, Moine L, Gehling VS, Brenneman J, Cantone N, Stuckey JI, Apte S, Ramakrishnan A, Bruderek K, Bradley WD, Audia JE, Cummings RT, Sims RJ 3rd, Trojer P, Levell JR. Khanna A, et al. Among authors: sims rj 3rd. ACS Med Chem Lett. 2020 Mar 26;11(6):1205-1212. doi: 10.1021/acsmedchemlett.0c00045. eCollection 2020 Jun 11. ACS Med Chem Lett. 2020. PMID: 32551002 Free PMC article.
Bromodomains: a new target class for drug development.
Cochran AG, Conery AR, Sims RJ 3rd. Cochran AG, et al. Among authors: sims rj 3rd. Nat Rev Drug Discov. 2019 Aug;18(8):609-628. doi: 10.1038/s41573-019-0030-7. Epub 2019 Jul 4. Nat Rev Drug Discov. 2019. PMID: 31273347 Review.
GNE-886: A Potent and Selective Inhibitor of the Cat Eye Syndrome Chromosome Region Candidate 2 Bromodomain (CECR2).
Crawford TD, Audia JE, Bellon S, Burdick DJ, Bommi-Reddy A, Côté A, Cummings RT, Duplessis M, Flynn EM, Hewitt M, Huang HR, Jayaram H, Jiang Y, Joshi S, Kiefer JR, Murray J, Nasveschuk CG, Neiss A, Pardo E, Romero FA, Sandy P, Sims RJ 3rd, Tang Y, Taylor AM, Tsui V, Wang J, Wang S, Wang Y, Xu Z, Zawadzke L, Zhu X, Albrecht BK, Magnuson SR, Cochran AG. Crawford TD, et al. Among authors: sims rj 3rd. ACS Med Chem Lett. 2017 Jun 1;8(7):737-741. doi: 10.1021/acsmedchemlett.7b00132. eCollection 2017 Jul 13. ACS Med Chem Lett. 2017. PMID: 28740608 Free PMC article.
57 results