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Page 1
The promise and peril of chemical probes.
Arrowsmith CH, Audia JE, Austin C, Baell J, Bennett J, Blagg J, Bountra C, Brennan PE, Brown PJ, Bunnage ME, Buser-Doepner C, Campbell RM, Carter AJ, Cohen P, Copeland RA, Cravatt B, Dahlin JL, Dhanak D, Edwards AM, Frederiksen M, Frye SV, Gray N, Grimshaw CE, Hepworth D, Howe T, Huber KV, Jin J, Knapp S, Kotz JD, Kruger RG, Lowe D, Mader MM, Marsden B, Mueller-Fahrnow A, Müller S, O'Hagan RC, Overington JP, Owen DR, Rosenberg SH, Roth B, Ross R, Schapira M, Schreiber SL, Shoichet B, Sundström M, Superti-Furga G, Taunton J, Toledo-Sherman L, Walpole C, Walters MA, Willson TM, Workman P, Young RN, Zuercher WJ. Arrowsmith CH, et al. Among authors: audia je. Nat Chem Biol. 2015 Aug;11(8):536-41. doi: 10.1038/nchembio.1867. Nat Chem Biol. 2015. PMID: 26196764 Free PMC article.
Corrigendum: The promise and peril of chemical probes.
Arrowsmith CH, Audia JE, Austin C, Baell J, Bennett J, Blagg J, Bountra C, Brennan PE, Brown PJ, Bunnage ME, Buser-Doepner C, Campbell RM, Carter AJ, Cohen P, Copeland RA, Cravatt B, Dahlin JL, Dhanak D, Edwards AM, Frederiksen M, Frye SV, Gray N, Grimshaw CE, Hepworth D, Howe T, Huber KV, Jin J, Knapp S, Kotz JD, Kruger RG, Lowe D, Mader MM, Marsden B, Mueller-Fahrnow A, Müller S, O'Hagan RC, Overington JP, Owen DR, Rosenberg SH, Ross R, Roth B, Schapira M, Schreiber SL, Shoichet B, Sundström M, Superti-Furga G, Taunton J, Toledo-Sherman L, Walpole C, Walters MA, Willson TM, Workman P, Young RN, Zuercher WJ. Arrowsmith CH, et al. Among authors: audia je. Nat Chem Biol. 2015 Nov;11(11):887. doi: 10.1038/nchembio1115-887c. Nat Chem Biol. 2015. PMID: 26485080 No abstract available.
Histone Modifications and Cancer.
Audia JE, Campbell RM. Audia JE, et al. Cold Spring Harb Perspect Biol. 2016 Apr 1;8(4):a019521. doi: 10.1101/cshperspect.a019521. Cold Spring Harb Perspect Biol. 2016. PMID: 27037415 Free PMC article. Review.
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
US immigration order strikes against biotech.
Levin JM, Holtzman SH, Maraganore J, Hastings PJ, Cohen R, Dahiyat B, Adams J, Adams C, Ahrens B, Albers J, Aspinall MG, Audia JE, Babler M, Barrett P, Barry Z, Bermingham N, Bloch S, Blum RI, Bolno PB, Bonney MW, Booth B, Bradbury DM, Brauer SK, Byers B, Cagnoni PJ, Cali BM, Ciechanover I, Clark C, Clayman MD, Cleland JL, Cobb P, Cooper R, Currie MG, Diekman J, Dobmeier EL, Doerfler D, Donley EL, Dunsire D, During M, Eckstein JW, Elenko E, Exter NA, Fleming JJ, Flesher GJ, Formela JF, Forrester R, Francois C, Franklin H, Freeman MW, Furst H, Gage LP, Galakatos N, Gallagher BM, Geraghty JA, Gill S, Goeddel DV, Goldsmith MA, Gowen M, Goyal V, Graney T, Grayzel D, Greene B, Grint P, Gutierrez-Ramos JC, Haney B, Ha-Ngoc T, Harris T, Hasnain F, Hata YS, Hecht P, Henshaw L, Heyman R, Hoppenot H, Horvitz HR, Hughes TE, Hutton WS, Isaacs ST, Jenkins A, Jonker J, Kaplan J, Karsen P, Keiper J, Kim J, Kindler J, King R, King V, Kjellson N, Koenig S, Koenig G, Kolchinsky P, Laikind P, Langer RB, Lee JJ, Leff JS, Leicher BA, Leschly N, Levin A, Levin M, Levine AJ, Levy A, Liu DR, Lodish HF, Lopatin U, Love TW, Macdonald G, Maderis GJ, Mahadevia A, Mahanthappa NK, Martin JF, Martin A, M… See abstract for full author list ➔ Levin JM, et al. Among authors: audia je. Nat Biotechnol. 2017 Mar 7;35(3):204-206. doi: 10.1038/nbt.3824. Nat Biotechnol. 2017. PMID: 28267733 No abstract available.
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
Discovery and Optimization of Tetramethylpiperidinyl Benzamides as Inhibitors of EZH2.
Nasveschuk CG, Gagnon A, Garapaty-Rao S, Balasubramanian S, Campbell R, Lee C, Zhao F, Bergeron L, Cummings R, Trojer P, Audia JE, Albrecht BK, Harmange JC. Nasveschuk CG, et al. Among authors: audia je. ACS Med Chem Lett. 2014 Jan 14;5(4):378-83. doi: 10.1021/ml400494b. eCollection 2014 Apr 10. ACS Med Chem Lett. 2014. PMID: 24900844 Free PMC article.
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: audia je. 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.
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.
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
61 results