Antagonism of c-IAP and XIAP Proteins Is Required for Efficient Induction of Cell Death by Small-Molecule IAP Antagonists

The inhibitor of apoptosis (IAP) proteins are critical regulators of cancer cell survival, which makes them attractive targets for therapeutic intervention in cancers. Herein, we describe the structure-based design of IAP antagonists with high affinities and selectivity (>2000-fold) for c-IAP1 ov...

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Veröffentlicht in:	ACS chemical biology 2009-07, Vol.4 (7), p.557-566
Hauptverfasser:	Ndubaku, Chudi, Varfolomeev, Eugene, Wang, Lan, Zobel, Kerry, Lau, Kevin, Elliott, Linda O, Maurer, Brigitte, Fedorova, Anna V, Dynek, Jasmin N, Koehler, Michael, Hymowitz, Sarah G, Tsui, Vickie, Deshayes, Kurt, Fairbrother, Wayne J, Flygare, John A, Vucic, Domagoj
Format:	Artikel
Sprache:	eng
Schlagworte:	Binding Sites Cell Death - drug effects Cell Line Humans Inhibitor of Apoptosis Proteins - antagonists & inhibitors Inhibitor of Apoptosis Proteins - chemistry Inhibitor of Apoptosis Proteins - metabolism Melanoma - pathology Models, Molecular Molecular Structure Neoplasms - drug therapy NF-kappa B - metabolism Protein Binding Structure-Activity Relationship X-Linked Inhibitor of Apoptosis Protein - antagonists & inhibitors
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