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Birinapant, a smac-mimetic with improved tolerability for the treatment of solid tumors and hematological malignancies.
Condon SM, Mitsuuchi Y, Deng Y, LaPorte MG, Rippin SR, Haimowitz T, Alexander MD, Kumar PT, Hendi MS, Lee YH, Benetatos CA, Yu G, Kapoor GS, Neiman E, Seipel ME, Burns JM, Graham MA, McKinlay MA, Li X, Wang J, Shi Y, Feltham R, Bettjeman B, Cumming MH, Vince JE, Khan N, Silke J, Day CL, Chunduru SK. Condon SM, et al. Among authors: kapoor gs. J Med Chem. 2014 May 8;57(9):3666-77. doi: 10.1021/jm500176w. Epub 2014 Apr 15. J Med Chem. 2014. PMID: 24684347
Birinapant (TL32711), a bivalent SMAC mimetic, targets TRAF2-associated cIAPs, abrogates TNF-induced NF-κB activation, and is active in patient-derived xenograft models.
Benetatos CA, Mitsuuchi Y, Burns JM, Neiman EM, Condon SM, Yu G, Seipel ME, Kapoor GS, Laporte MG, Rippin SR, Deng Y, Hendi MS, Tirunahari PK, Lee YH, Haimowitz T, Alexander MD, Graham MA, Weng D, Shi Y, McKinlay MA, Chunduru SK. Benetatos CA, et al. Among authors: kapoor gs. Mol Cancer Ther. 2014 Apr;13(4):867-79. doi: 10.1158/1535-7163.MCT-13-0798. Epub 2014 Feb 21. Mol Cancer Ther. 2014. PMID: 24563541
Bivalent IAP antagonists, but not monovalent IAP antagonists, inhibit TNF-mediated NF-κB signaling by degrading TRAF2-associated cIAP1 in cancer cells.
Mitsuuchi Y, Benetatos CA, Deng Y, Haimowitz T, Beck SC, Arnone MR, Kapoor GS, Seipel ME, Chunduru SK, McKinlay MA, Begley CG, Condon SM. Mitsuuchi Y, et al. Among authors: kapoor gs. Cell Death Discov. 2017 Jan 16;3:16046. doi: 10.1038/cddiscovery.2016.46. eCollection 2017. Cell Death Discov. 2017. PMID: 28149532 Free PMC article.
Mitogenic signaling cascades in glial tumors.
Kapoor GS, O'Rourke DM. Kapoor GS, et al. Neurosurgery. 2003 Jun;52(6):1425-34; discussion 1434-5. doi: 10.1227/01.neu.0000065135.28143.39. Neurosurgery. 2003. PMID: 12762887 Review.
27 results