Ontology highlight
ABSTRACT:
SUBMITTER: Sun H
PROVIDER: S-EPMC2553712 | biostudies-literature | 2007 Dec
REPOSITORIES: biostudies-literature
Sun Haiying H Nikolovska-Coleska Zaneta Z Lu Jianfeng J Meagher Jennifer L JL Yang Chao-Yie CY Qiu Su S Tomita York Y Ueda Yumi Y Jiang Sheng S Krajewski Krzysztof K Roller Peter P PP Stuckey Jeanne A JA Wang Shaomeng S
Journal of the American Chemical Society 20071114 49
XIAP is a central apoptosis regulator that inhibits apoptosis by binding to and inhibiting the effectors caspase-3/-7 and an initiator caspase-9 through its BIR2 and BIR3 domains, respectively. Smac protein in its dimeric form effectively antagonizes XIAP by concurrently targeting both its BIR2 and BIR3 domains. We report the design, synthesis, and characterization of a nonpeptide, cell-permeable, bivalent small-molecule (SM-164) which mimics Smac protein for targeting XIAP. Our study shows that ...[more]