Design, Synthesis and Characterization of A Potent, Non-Peptide, Cell-Permeable, Bivalent Smac Mimetic that Concurrently Targets both the BIR2 and BIR3 Domains in XIAP

(A). A schematic, simplified apoptosis pathway. XIAP inhibits apoptosis by directly binding to and inhibition of caspase-9, caspase-3 and -7. Smac protein binds to XIAP and antagonizes XIAP to promote activation of caspases and apoptosis. (B). Design of bivalent Smac mimetics to target both the BIR2 and BIR3 domains of XIAP by mimicking the binding of dimeric Smac protein.

Publication

Design, Synthesis and Characterization of A Potent, Non-Peptide, Cell-Permeable, Bivalent Smac Mimetic that Concurrently Targets both the BIR2 and BIR3 Domains in XIAP. () Haiying Sun, et al. J Am Chem Soc. ;129(49):15279-15294. Figure: F1. Homo sapiens

Disease mentions