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Page 1
A Method for Determining the Kinetics of Small-Molecule-Induced Ubiquitination.
Vieux EF, Agafonov RV, Emerson L, Isasa M, Deibler RW, Simard JR, Cocozziello D, Ladd B, Lee L, Li H, Archer S, Fitzgerald M, Michael R, Nasveschuk CG, Park ES, Kern G, Proia DA, Phillips AJ, Fisher SL. Vieux EF, et al. Among authors: nasveschuk cg. SLAS Discov. 2021 Apr;26(4):547-559. doi: 10.1177/24725552211000673. SLAS Discov. 2021. PMID: 33780296 Free article.
Evaluation of the Small-molecule BRD4 Degrader CFT-2718 in Small-cell Lung Cancer and Pancreatic Cancer Models.
Sun D, Nikonova AS, Zhang P, Deneka AY, Fitzgerald ME, Michael RE, Lee L, Lilly AC, Fisher SL, Phillips AJ, Nasveschuk CG, Proia DA, Tu Z, Golemis EA. Sun D, et al. Among authors: nasveschuk cg. Mol Cancer Ther. 2021 Aug;20(8):1367-1377. doi: 10.1158/1535-7163.MCT-20-0831. Epub 2021 May 27. Mol Cancer Ther. 2021. PMID: 34045230 Free PMC article.
Structural Characterization of Degrader-Induced Ternary Complexes Using Hydrogen-Deuterium Exchange Mass Spectrometry and Computational Modeling: Implications for Structure-Based Design.
Eron SJ, Huang H, Agafonov RV, Fitzgerald ME, Patel J, Michael RE, Lee TD, Hart AA, Shaulsky J, Nasveschuk CG, Phillips AJ, Fisher SL, Good A. Eron SJ, et al. Among authors: nasveschuk cg. ACS Chem Biol. 2021 Nov 19;16(11):2228-2243. doi: 10.1021/acschembio.1c00376. Epub 2021 Sep 28. ACS Chem Biol. 2021. PMID: 34582690 Free article.
Identification and mechanistic studies of a novel ubiquitin E1 inhibitor.
Ungermannova D, Parker SJ, Nasveschuk CG, Chapnick DA, Phillips AJ, Kuchta RD, Liu X. Ungermannova D, et al. Among authors: nasveschuk cg. J Biomol Screen. 2012 Apr;17(4):421-34. doi: 10.1177/1087057111433843. Epub 2012 Jan 24. J Biomol Screen. 2012. PMID: 22274912 Free PMC article.
Preclinical Development of the Class-I-Selective Histone Deacetylase Inhibitor OKI-179 for the Treatment of Solid Tumors.
Diamond JR, Pitts TM, Ungermannova D, Nasveschuk CG, Zhang G, Phillips AJ, Bagby SM, Pafford J, Yacob BW, Newton TP, Tentler JJ, Gittleman B, Hartman SJ, DeMattei JA, Winkler JD, Wendt MK, Schiemann WP, Eckhardt SG, Liu X, Piscopio AD. Diamond JR, et al. Among authors: nasveschuk cg. Mol Cancer Ther. 2022 Mar 1;21(3):397-406. doi: 10.1158/1535-7163.MCT-21-0455. Mol Cancer Ther. 2022. PMID: 34965958 Free PMC article.
Diving into the Water: Inducible Binding Conformations for BRD4, TAF1(2), BRD9, and CECR2 Bromodomains.
Crawford TD, Tsui V, Flynn EM, Wang S, Taylor AM, Côté A, Audia JE, Beresini MH, Burdick DJ, Cummings R, Dakin LA, Duplessis M, Good AC, Hewitt MC, Huang HR, Jayaram H, Kiefer JR, Jiang Y, Murray J, Nasveschuk CG, Pardo E, Poy F, Romero FA, Tang Y, Wang J, Xu Z, Zawadzke LE, Zhu X, Albrecht BK, Magnuson SR, Bellon S, Cochran AG. Crawford TD, et al. Among authors: nasveschuk cg. J Med Chem. 2016 Jun 9;59(11):5391-402. doi: 10.1021/acs.jmedchem.6b00264. Epub 2016 May 31. J Med Chem. 2016. PMID: 27219867
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: nasveschuk cg. 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-064: A Potent, Selective, and Orally Bioavailable Chemical Probe for the Bromodomains of SMARCA2 and SMARCA4 and the Fifth Bromodomain of PBRM1.
Taylor AM, Bailey C, Belmont LD, Campbell R, Cantone N, Côté A, Crawford TD, Cummings R, DeMent K, Duplessis M, Flynn M, Good AC, Huang HR, Joshi S, Leblanc Y, Murray J, Nasveschuk CG, Neiss A, Poy F, Romero FA, Sandy P, Tang Y, Tsui V, Zawadzke L, Sims RJ 3rd, Audia JE, Bellon SF, Magnuson SR, Albrecht BK, Cochran AG. Taylor AM, et al. Among authors: nasveschuk cg. J Med Chem. 2022 Aug 25;65(16):11177-11186. doi: 10.1021/acs.jmedchem.2c00662. Epub 2022 Aug 5. J Med Chem. 2022. PMID: 35930799
29 results