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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: jackson jr. 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 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: jackson jr. 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.
Novel ATP-competitive kinesin spindle protein inhibitors.
Parrish CA, Adams ND, Auger KR, Burgess JL, Carson JD, Chaudhari AM, Copeland RA, Diamond MA, Donatelli CA, Duffy KJ, Faucette LF, Finer JT, Huffman WF, Hugger ED, Jackson JR, Knight SD, Luo L, Moore ML, Newlander KA, Ridgers LH, Sakowicz R, Shaw AN, Sung CM, Sutton D, Wood KW, Zhang SY, Zimmerman MN, Dhanak D. Parrish CA, et al. Among authors: jackson jr. J Med Chem. 2007 Oct 4;50(20):4939-52. doi: 10.1021/jm070435y. Epub 2007 Aug 29. J Med Chem. 2007. PMID: 17725339
ATP-competitive inhibitors of the mitotic kinesin KSP that function via an allosteric mechanism.
Luo L, Parrish CA, Nevins N, McNulty DE, Chaudhari AM, Carson JD, Sudakin V, Shaw AN, Lehr R, Zhao H, Sweitzer S, Lad L, Wood KW, Sakowicz R, Annan RS, Huang PS, Jackson JR, Dhanak D, Copeland RA, Auger KR. Luo L, et al. Among authors: jackson jr. Nat Chem Biol. 2007 Nov;3(11):722-6. doi: 10.1038/nchembio.2007.34. Epub 2007 Oct 7. Nat Chem Biol. 2007. PMID: 17922005
Sensitivity of cancer cells to Plk1 inhibitor GSK461364A is associated with loss of p53 function and chromosome instability.
Degenhardt Y, Greshock J, Laquerre S, Gilmartin AG, Jing J, Richter M, Zhang X, Bleam M, Halsey W, Hughes A, Moy C, Liu-Sullivan N, Powers S, Bachman K, Jackson J, Weber B, Wooster R. Degenhardt Y, et al. Mol Cancer Ther. 2010 Jul;9(7):2079-89. doi: 10.1158/1535-7163.MCT-10-0095. Epub 2010 Jun 22. Mol Cancer Ther. 2010. PMID: 20571075
Conformation-dependent ligand regulation of ATP hydrolysis by human KSP: activation of basal hydrolysis and inhibition of microtubule-stimulated hydrolysis by a single, small molecule modulator.
Luo L, Carson JD, Molnar KS, Tuske SJ, Coales SJ, Hamuro Y, Sung CM, Sudakin V, Auger KR, Dhanak D, Jackson JR, Huang PS, Tummino PJ, Copeland RA. Luo L, et al. Among authors: jackson jr. J Am Chem Soc. 2008 Jun 18;130(24):7584-91. doi: 10.1021/ja710889h. Epub 2008 May 21. J Am Chem Soc. 2008. PMID: 18491908
Distinct concentration-dependent effects of the polo-like kinase 1-specific inhibitor GSK461364A, including differential effect on apoptosis.
Gilmartin AG, Bleam MR, Richter MC, Erskine SG, Kruger RG, Madden L, Hassler DF, Smith GK, Gontarek RR, Courtney MP, Sutton D, Diamond MA, Jackson JR, Laquerre SG. Gilmartin AG, et al. Among authors: jackson jr. Cancer Res. 2009 Sep 1;69(17):6969-77. doi: 10.1158/0008-5472.CAN-09-0945. Epub 2009 Aug 18. Cancer Res. 2009. PMID: 19690138
496 results