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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
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
A Biparatopic Antibody-Drug Conjugate to Treat MET-Expressing Cancers, Including Those that Are Unresponsive to MET Pathway Blockade.
DaSilva JO, Yang K, Surriga O, Nittoli T, Kunz A, Franklin MC, Delfino FJ, Mao S, Zhao F, Giurleo JT, Kelly MP, Makonnen S, Hickey C, Krueger P, Foster R, Chen Z, Retter MW, Slim R, Young TM, Olson WC, Thurston G, Daly C. DaSilva JO, et al. Among authors: zhao f. Mol Cancer Ther. 2021 Oct;20(10):1966-1976. doi: 10.1158/1535-7163.MCT-21-0009. Epub 2021 Jul 26. Mol Cancer Ther. 2021. PMID: 34315762 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: 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.
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
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
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.
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