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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: zhao f. 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 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: zhao f. 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 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: zhao f. 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.
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: zhao f. Chem Biol. 2014 Nov 20;21(11):1463-75. doi: 10.1016/j.chembiol.2014.09.017. Chem Biol. 2014. PMID: 25457180
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: zhao f. 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.
An Alternative Approach to ChIP-Seq Normalization Enables Detection of Genome-Wide Changes in Histone H3 Lysine 27 Trimethylation upon EZH2 Inhibition.
Egan B, Yuan CC, Craske ML, Labhart P, Guler GD, Arnott D, Maile TM, Busby J, Henry C, Kelly TK, Tindell CA, Jhunjhunwala S, Zhao F, Hatton C, Bryant BM, Classon M, Trojer P. Egan B, et al. Among authors: zhao f. PLoS One. 2016 Nov 22;11(11):e0166438. doi: 10.1371/journal.pone.0166438. eCollection 2016. PLoS One. 2016. PMID: 27875550 Free PMC article.
Comprehensive Target Engagement by the EZH2 Inhibitor Tulmimetostat Allows for Targeting of ARID1A Mutant Cancers.
Keller PJ, Adams EJ, Wu R, Côté A, Arora S, Cantone N, Meyer R, Mertz JA, Gehling V, Cui J, Stuckey JI, Khanna A, Zhao F, Chen Z, Yu Z, Cummings RT, Taimi M, Lakhani NJ, Rasco D, Gutierrez M, Duska L, Devitt M, Rippley R, Levell J, Truong J, Wang J, Sun K, Trojer P. Keller PJ, et al. Among authors: zhao f. Cancer Res. 2024 Aug 1;84(15):2501-2517. doi: 10.1158/0008-5472.CAN-24-0398. Cancer Res. 2024. PMID: 38833522 Free PMC article. Clinical Trial.
Antibody drug conjugates of cleavable amino-alkyl and aryl maytansinoids.
Nittoli T, Kelly MP, Delfino F, Rudge J, Kunz A, Markotan T, Spink J, Chen Z, Shan J, Navarro E, Tait M, Provoncha K, Giurleo J, Zhao F, Jiang X, Hylton D, Makonnen S, Hickey C, Kirshner JR, Thurston G, Papadopoulos N. Nittoli T, et al. Among authors: zhao f. Bioorg Med Chem. 2018 May 15;26(9):2271-2279. doi: 10.1016/j.bmc.2018.02.025. Epub 2018 Feb 21. Bioorg Med Chem. 2018. PMID: 29605304
Antibody drug conjugates of cleavable amino-benzoyl-maytansinoids.
Nittoli T, Delfino F, Kelly M, Carosso S, Markotan T, Kunz A, Chen Z, Mao S, Shan J, Navarro E, Zhao F, Makonnen S, Hickey C, Spink J, Olson W, Kirshner JR, Thurston G, Papadopoulos N. Nittoli T, et al. Among authors: zhao f. Bioorg Med Chem. 2020 Dec 1;28(23):115785. doi: 10.1016/j.bmc.2020.115785. Epub 2020 Oct 11. Bioorg Med Chem. 2020. PMID: 33099182
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