Design, synthesis, and biological activity of a potent Smac mimetic that sensitizes cancer cells to apoptosis by antagonizing IAPs.

@article{Zobel2006DesignSA,
  title={Design, synthesis, and biological activity of a potent Smac mimetic that sensitizes cancer cells to apoptosis by antagonizing IAPs.},
  author={Kerry Zobel and Lan Wang and Eugene Varfolomeev and Matthew C. Franklin and Linda O. Elliott and Heidi A Wallweber and David C Okawa and John A. Flygare and Domagoj Vucic and Wayne J. Fairbrother and Kurt D Deshayes},
  journal={ACS chemical biology},
  year={2006},
  volume={1 8},
  pages={525-33}
}
Designed second mitochondrial activator of caspases (Smac) mimetics based on an accessible [7,5]-bicyclic scaffold bind to and antagonize protein interactions involving the inhibitor of apoptosis (IAP) proteins, X-chromosome-linked IAP (XIAP), melanoma IAP (ML-IAP), and c-IAPs 1 and 2 (cIAP1 and cIAP2). The design rationale is based on a combination of phage-panning data, peptide binding studies, and a survey of potential isosteres. The synthesis of two scaffolds is described. These compounds… CONTINUE READING

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