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Discovery of GSK1070916, a potent and selective inhibitor of Aurora B/C kinase.
Adams ND, Adams JL, Burgess JL, Chaudhari AM, Copeland RA, Donatelli CA, Drewry DH, Fisher KE, Hamajima T, Hardwicke MA, Huffman WF, Koretke-Brown KK, Lai ZV, McDonald OB, Nakamura H, Newlander KA, Oleykowski CA, Parrish CA, Patrick DR, Plant R, Sarpong MA, Sasaki K, Schmidt SJ, Silva DJ, Sutton D, Tang J, Thompson CS, Tummino PJ, Wang JC, Xiang H, Yang J, Dhanak D. Adams ND, et al. Among authors: yang j. J Med Chem. 2010 May 27;53(10):3973-4001. doi: 10.1021/jm901870q. J Med Chem. 2010. PMID: 20420387
Binding of TPX2 to Aurora A alters substrate and inhibitor interactions.
Anderson K, Yang J, Koretke K, Nurse K, Calamari A, Kirkpatrick RB, Patrick D, Silva D, Tummino PJ, Copeland RA, Lai Z. Anderson K, et al. Among authors: yang j. Biochemistry. 2007 Sep 11;46(36):10287-95. doi: 10.1021/bi7011355. Epub 2007 Aug 18. Biochemistry. 2007. PMID: 17705509
GSK1838705A inhibits the insulin-like growth factor-1 receptor and anaplastic lymphoma kinase and shows antitumor activity in experimental models of human cancers.
Sabbatini P, Korenchuk S, Rowand JL, Groy A, Liu Q, Leperi D, Atkins C, Dumble M, Yang J, Anderson K, Kruger RG, Gontarek RR, Maksimchuk KR, Suravajjala S, Lapierre RR, Shotwell JB, Wilson JW, Chamberlain SD, Rabindran SK, Kumar R. Sabbatini P, et al. Among authors: yang j. Mol Cancer Ther. 2009 Oct;8(10):2811-20. doi: 10.1158/1535-7163.MCT-09-0423. Mol Cancer Ther. 2009. PMID: 19825801
GSK1120212 (JTP-74057) is an inhibitor of MEK activity and activation with favorable pharmacokinetic properties for sustained in vivo pathway inhibition.
Gilmartin AG, Bleam MR, Groy A, Moss KG, Minthorn EA, Kulkarni SG, Rominger CM, Erskine S, Fisher KE, Yang J, Zappacosta F, Annan R, Sutton D, Laquerre SG. Gilmartin AG, et al. Among authors: yang j. Clin Cancer Res. 2011 Mar 1;17(5):989-1000. doi: 10.1158/1078-0432.CCR-10-2200. Epub 2011 Jan 18. Clin Cancer Res. 2011. PMID: 21245089
Dabrafenib; preclinical characterization, increased efficacy when combined with trametinib, while BRAF/MEK tool combination reduced skin lesions.
King AJ, Arnone MR, Bleam MR, Moss KG, Yang J, Fedorowicz KE, Smitheman KN, Erhardt JA, Hughes-Earle A, Kane-Carson LS, Sinnamon RH, Qi H, Rheault TR, Uehling DE, Laquerre SG. King AJ, et al. Among authors: yang j. PLoS One. 2013 Jul 3;8(7):e67583. doi: 10.1371/journal.pone.0067583. Print 2013. PLoS One. 2013. PMID: 23844038 Free PMC article.
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