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Page 1
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: normant e. 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: normant e. 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
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: normant e. 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.
EZH2 inhibitor efficacy in non-Hodgkin's lymphoma does not require suppression of H3K27 monomethylation.
Bradley WD, Arora S, Busby J, Balasubramanian S, Gehling VS, Nasveschuk CG, Vaswani RG, Yuan CC, Hatton C, Zhao F, Williamson KE, Iyer P, Méndez J, Campbell R, Cantone N, Garapaty-Rao S, Audia JE, Cook AS, Dakin LA, Albrecht BK, Harmange JC, Daniels DL, Cummings RT, Bryant BM, Normant E, Trojer P. Bradley WD, et al. Among authors: normant e. Chem Biol. 2014 Nov 20;21(11):1463-75. doi: 10.1016/j.chembiol.2014.09.017. Chem Biol. 2014. PMID: 25457180
Hsp90 (heat shock protein 90) inhibitor occupancy is a direct determinant of client protein degradation and tumor growth arrest in vivo.
Tillotson B, Slocum K, Coco J, Whitebread N, Thomas B, West KA, MacDougall J, Ge J, Ali JA, Palombella VJ, Normant E, Adams J, Fritz CC. Tillotson B, et al. Among authors: normant e. J Biol Chem. 2010 Dec 17;285(51):39835-43. doi: 10.1074/jbc.M110.141580. Epub 2010 Oct 12. J Biol Chem. 2010. PMID: 20940293 Free PMC article.
Blockade of oncogenic IκB kinase activity in diffuse large B-cell lymphoma by bromodomain and extraterminal domain protein inhibitors.
Ceribelli M, Kelly PN, Shaffer AL, Wright GW, Xiao W, Yang Y, Mathews Griner LA, Guha R, Shinn P, Keller JM, Liu D, Patel PR, Ferrer M, Joshi S, Nerle S, Sandy P, Normant E, Thomas CJ, Staudt LM. Ceribelli M, et al. Among authors: normant e. Proc Natl Acad Sci U S A. 2014 Aug 5;111(31):11365-70. doi: 10.1073/pnas.1411701111. Epub 2014 Jul 21. Proc Natl Acad Sci U S A. 2014. PMID: 25049379 Free PMC article.
Development of 17-allylamino-17-demethoxygeldanamycin hydroquinone hydrochloride (IPI-504), an anti-cancer agent directed against Hsp90.
Sydor JR, Normant E, Pien CS, Porter JR, Ge J, Grenier L, Pak RH, Ali JA, Dembski MS, Hudak J, Patterson J, Penders C, Pink M, Read MA, Sang J, Woodward C, Zhang Y, Grayzel DS, Wright J, Barrett JA, Palombella VJ, Adams J, Tong JK. Sydor JR, et al. Among authors: normant e. Proc Natl Acad Sci U S A. 2006 Nov 14;103(46):17408-13. doi: 10.1073/pnas.0608372103. Epub 2006 Nov 7. Proc Natl Acad Sci U S A. 2006. PMID: 17090671 Free PMC article.
42 results