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Page 1
Identification of potent, selective KDM5 inhibitors.
Gehling VS, Bellon SF, Harmange JC, LeBlanc Y, Poy F, Odate S, Buker S, Lan F, Arora S, Williamson KE, Sandy P, Cummings RT, Bailey CM, Bergeron L, Mao W, Gustafson A, Liu Y, VanderPorten E, Audia JE, Trojer P, Albrecht BK. Gehling VS, et al. Among authors: audia je. Bioorg Med Chem Lett. 2016 Sep 1;26(17):4350-4. doi: 10.1016/j.bmcl.2016.07.026. Epub 2016 Jul 19. Bioorg Med Chem Lett. 2016. PMID: 27476424
Identification of EZH2 and EZH1 small molecule inhibitors with selective impact on diffuse large B cell lymphoma cell growth.
Garapaty-Rao S, Nasveschuk C, Gagnon A, Chan EY, Sandy P, Busby J, Balasubramanian S, Campbell R, Zhao F, Bergeron L, Audia JE, Albrecht BK, Harmange JC, Cummings R, Trojer P. Garapaty-Rao S, et al. Among authors: audia je. Chem Biol. 2013 Nov 21;20(11):1329-39. doi: 10.1016/j.chembiol.2013.09.013. Epub 2013 Oct 31. Chem Biol. 2013. PMID: 24183969
Discovery, Design, and Optimization of Isoxazole Azepine BET Inhibitors.
Gehling VS, Hewitt MC, Vaswani RG, Leblanc Y, Côté A, Nasveschuk CG, Taylor AM, Harmange JC, Audia JE, Pardo E, Joshi S, Sandy P, Mertz JA, Sims RJ 3rd, Bergeron L, Bryant BM, Bellon S, Poy F, Jayaram H, Sankaranarayanan R, Yellapantula S, Bangalore Srinivasamurthy N, Birudukota S, Albrecht BK. Gehling VS, et al. Among authors: audia je. ACS Med Chem Lett. 2013 Jul 16;4(9):835-40. doi: 10.1021/ml4001485. eCollection 2013 Sep 12. ACS Med Chem Lett. 2013. PMID: 24900758 Free PMC article.
Development of methyl isoxazoleazepines as inhibitors of BET.
Hewitt MC, Leblanc Y, Gehling VS, Vaswani RG, Côté A, Nasveschuk CG, Taylor AM, Harmange JC, Audia JE, Pardo E, Cummings R, Joshi S, Sandy P, Mertz JA, Sims RJ 3rd, Bergeron L, Bryant BM, Bellon S, Poy F, Jayaram H, Tang Y, Albrecht BK. Hewitt MC, et al. Among authors: audia je. Bioorg Med Chem Lett. 2015 May 1;25(9):1842-8. doi: 10.1016/j.bmcl.2015.03.045. Epub 2015 Mar 24. Bioorg Med Chem Lett. 2015. PMID: 25851940
Discovery, design, and synthesis of indole-based EZH2 inhibitors.
Gehling VS, Vaswani RG, Nasveschuk CG, Duplessis M, Iyer P, Balasubramanian S, Zhao F, Good AC, Campbell R, Lee C, Dakin LA, Cook AS, Gagnon A, Harmange JC, Audia JE, Cummings RT, Normant E, Trojer P, Albrecht BK. Gehling VS, et al. Among authors: audia je. Bioorg Med Chem Lett. 2015 Sep 1;25(17):3644-9. doi: 10.1016/j.bmcl.2015.06.056. Epub 2015 Jun 19. Bioorg Med Chem Lett. 2015. PMID: 26189078
Identification of a Benzoisoxazoloazepine Inhibitor (CPI-0610) of the Bromodomain and Extra-Terminal (BET) Family as a Candidate for Human Clinical Trials.
Albrecht BK, Gehling VS, Hewitt MC, Vaswani RG, Côté A, Leblanc Y, Nasveschuk CG, Bellon S, Bergeron L, Campbell R, Cantone N, Cooper MR, Cummings RT, Jayaram H, Joshi S, Mertz JA, Neiss A, Normant E, O'Meara M, Pardo E, Poy F, Sandy P, Supko J, Sims RJ 3rd, Harmange JC, Taylor AM, Audia JE. Albrecht BK, et al. Among authors: audia je. J Med Chem. 2016 Feb 25;59(4):1330-9. doi: 10.1021/acs.jmedchem.5b01882. Epub 2016 Feb 4. J Med Chem. 2016. PMID: 26815195
Discovery of Benzotriazolo[4,3-d][1,4]diazepines as Orally Active Inhibitors of BET Bromodomains.
Taylor AM, Vaswani RG, Gehling VS, Hewitt MC, Leblanc Y, Audia JE, Bellon S, Cummings RT, Côté A, Harmange JC, Jayaram H, Joshi S, Lora JM, Mertz JA, Neiss A, Pardo E, Nasveschuk CG, Poy F, Sandy P, Setser JW, Sims RJ 3rd, Tang Y, Albrecht BK. Taylor AM, et al. Among authors: audia je. ACS Med Chem Lett. 2015 Mar 25;7(2):145-50. doi: 10.1021/ml500411h. eCollection 2016 Feb 11. ACS Med Chem Lett. 2015. PMID: 26985289 Free PMC article.
Identification of (R)-N-((4-Methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1-(1-(1-(2,2,2-trifluoroethyl)piperidin-4-yl)ethyl)-1H-indole-3-carboxamide (CPI-1205), a Potent and Selective Inhibitor of Histone Methyltransferase EZH2, Suitable for Phase I Clinical Trials for B-Cell Lymphomas.
Vaswani RG, Gehling VS, Dakin LA, Cook AS, Nasveschuk CG, Duplessis M, Iyer P, Balasubramanian S, Zhao F, Good AC, Campbell R, Lee C, Cantone N, Cummings RT, Normant E, Bellon SF, Albrecht BK, Harmange JC, Trojer P, Audia JE, Zhang Y, Justin N, Chen S, Wilson JR, Gamblin SJ. Vaswani RG, et al. Among authors: audia je. J Med Chem. 2016 Nov 10;59(21):9928-9941. doi: 10.1021/acs.jmedchem.6b01315. Epub 2016 Oct 28. J Med Chem. 2016. PMID: 27739677 Free PMC article.
GNE-371, a Potent and Selective Chemical Probe for the Second Bromodomains of Human Transcription-Initiation-Factor TFIID Subunit 1 and Transcription-Initiation-Factor TFIID Subunit 1-like.
Wang S, Tsui V, Crawford TD, Audia JE, Burdick DJ, Beresini MH, Côté A, Cummings R, Duplessis M, Flynn EM, Hewitt MC, Huang HR, Jayaram H, Jiang Y, Joshi S, Murray J, Nasveschuk CG, Pardo E, Poy F, Romero FA, Tang Y, Taylor AM, Wang J, Xu Z, Zawadzke LE, Zhu X, Albrecht BK, Magnuson SR, Bellon S, Cochran AG. Wang S, et al. Among authors: audia je. J Med Chem. 2018 Oct 25;61(20):9301-9315. doi: 10.1021/acs.jmedchem.8b01225. Epub 2018 Oct 5. J Med Chem. 2018. PMID: 30289257
Design and Synthesis of Styrenylcyclopropylamine LSD1 Inhibitors.
Gehling VS, McGrath JP, Duplessis M, Khanna A, Brucelle F, Vaswani RG, Côté A, Stuckey J, Watson V, Cummings RT, Balasubramanian S, Iyer P, Sawant P, Good AC, Albrecht BK, Harmange JC, Audia JE, Bellon SF, Trojer P, Levell JR. Gehling VS, et al. Among authors: audia je. ACS Med Chem Lett. 2020 May 6;11(6):1213-1220. doi: 10.1021/acsmedchemlett.0c00060. eCollection 2020 Jun 11. ACS Med Chem Lett. 2020. PMID: 32551003 Free PMC article.
61 results