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Discovery of the First Potent and Selective Inhibitor of Centromere-Associated Protein E: GSK923295.
Qian X, McDonald A, Zhou HJ, Adams ND, Parrish CA, Duffy KJ, Fitch DM, Tedesco R, Ashcraft LW, Yao B, Jiang H, Huang JK, Marin MV, Aroyan CE, Wang J, Ahmed S, Burgess JL, Chaudhari AM, Donatelli CA, Darcy MG, Ridgers LH, Newlander KA, Schmidt SJ, Chai D, Colón M, Zimmerman MN, Lad L, Sakowicz R, Schauer S, Belmont L, Baliga R, Pierce DW, Finer JT, Wang Z, Morgan BP, Morgans DJ Jr, Auger KR, Sung CM, Carson JD, Luo L, Hugger ED, Copeland RA, Sutton D, Elliott JD, Jackson JR, Wood KW, Dhanak D, Bergnes G, Knight SD. Qian X, et al. Among authors: belmont l. ACS Med Chem Lett. 2010 Jan 19;1(1):30-4. doi: 10.1021/ml900018m. eCollection 2010 Apr 8. ACS Med Chem Lett. 2010. PMID: 24900171 Free PMC article.
Antitumor activity of an allosteric inhibitor of centromere-associated protein-E.
Wood KW, Lad L, Luo L, Qian X, Knight SD, Nevins N, Brejc K, Sutton D, Gilmartin AG, Chua PR, Desai R, Schauer SP, McNulty DE, Annan RS, Belmont LD, Garcia C, Lee Y, Diamond MA, Faucette LF, Giardiniere M, Zhang S, Sun CM, Vidal JD, Lichtsteiner S, Cornwell WD, Greshock JD, Wooster RF, Finer JT, Copeland RA, Huang PS, Morgans DJ Jr, Dhanak D, Bergnes G, Sakowicz R, Jackson JR. Wood KW, et al. Among authors: belmont ld. Proc Natl Acad Sci U S A. 2010 Mar 30;107(13):5839-44. doi: 10.1073/pnas.0915068107. Epub 2010 Feb 18. Proc Natl Acad Sci U S A. 2010. PMID: 20167803 Free PMC article.
Discovery of GDC-0853: A Potent, Selective, and Noncovalent Bruton's Tyrosine Kinase Inhibitor in Early Clinical Development.
Crawford JJ, Johnson AR, Misner DL, Belmont LD, Castanedo G, Choy R, Coraggio M, Dong L, Eigenbrot C, Erickson R, Ghilardi N, Hau J, Katewa A, Kohli PB, Lee W, Lubach JW, McKenzie BS, Ortwine DF, Schutt L, Tay S, Wei B, Reif K, Liu L, Wong H, Young WB. Crawford JJ, et al. Among authors: belmont ld. J Med Chem. 2018 Mar 22;61(6):2227-2245. doi: 10.1021/acs.jmedchem.7b01712. Epub 2018 Feb 23. J Med Chem. 2018. PMID: 29457982
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: belmont ld. 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
Insight into the molecular mechanism of the multitasking kinesin-8 motor.
Peters C, Brejc K, Belmont L, Bodey AJ, Lee Y, Yu M, Guo J, Sakowicz R, Hartman J, Moores CA. Peters C, et al. Among authors: belmont l. EMBO J. 2010 Oct 20;29(20):3437-47. doi: 10.1038/emboj.2010.220. Epub 2010 Sep 3. EMBO J. 2010. PMID: 20818331 Free PMC article.
Battling Btk Mutants With Noncovalent Inhibitors That Overcome Cys481 and Thr474 Mutations.
Johnson AR, Kohli PB, Katewa A, Gogol E, Belmont LD, Choy R, Penuel E, Burton L, Eigenbrot C, Yu C, Ortwine DF, Bowman K, Franke Y, Tam C, Estevez A, Mortara K, Wu J, Li H, Lin M, Bergeron P, Crawford JJ, Young WB. Johnson AR, et al. Among authors: belmont ld. ACS Chem Biol. 2016 Oct 21;11(10):2897-2907. doi: 10.1021/acschembio.6b00480. Epub 2016 Sep 7. ACS Chem Biol. 2016. PMID: 27571029
87 results