The Discovery of a Potent Small-Molecule Antagonist of Inhibitor of Apoptosis (IAP) Proteins and Clinical Candidate for the Treatment of Cancer (GDC-0152)

A series of compounds were designed and synthesized as antagonists of cIAP1/2, ML-IAP, and XIAP based on the N-terminus, AVPI, of mature Smac. Compound 1 (GDC-0152) has the best profile of these compounds; it binds to the XIAP BIR3 domain, the BIR domain of ML-IAP, and the BIR3 domains of cIAP1 and...

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Päätekijät: Flygare, John A., Beresini, Maureen, Budha, Nageshwar, Chan, Helen, Chan, Iris T., Cheeti, Sravanthi, Cohen, Frederick, Deshayes, Kurt, Doerner, Karl, Eckhardt, S. Gail, Elliott, Linda O., Feng, Bainian, Franklin, Matthew C., Reisner, Stacy Frankovitz, Gazzard, Lewis, Halladay, Jason, Hymowitz, Sarah G., La, Hank, LoRusso, Patricia, Maurer, Brigitte, Murray, Lesley, Plise, Emile, Quan, Clifford, Stephan, Jean-Philippe, Shin, Young G., Tom, Jeffrey, Tsui, Vickie, Um, Joanne, Varfolomeev, Eugene, Vucic, Domagoj, Wagner, Andrew J., Wallweber, Heidi J.A., Wang, Lan, Ware, Joseph, Wen, Zhaoyang, Wong, Harvey, Wong, Jonathan M., Wong, Melisa, Wong, Susan, Yu, Ron, Zobel, Kerry, Fairbrother, Wayne J.
Aineistotyyppi: Artigo
Kieli:Inglês
Julkaistu: 2012
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Article
Linkit:https://ncbi.nlm.nih.gov/pmc/articles/PMC3366583/
https://ncbi.nlm.nih.gov/pubmed/22413863
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/jm300060k
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