Unknown

Dataset Information

0

Development of Peptidomimetics Targeting IAPs.


ABSTRACT: Inhibitor of apoptosis proteins (IAPs) such as XIAP subvert apoptosis by binding and inhibiting caspases. Because occupation of the XIAP BIR3 peptide binding pocket by Smac abolishes the XIAP-caspase 9 interaction, it is a proapoptotic event of great therapeutic interest. An assay for pocket binding was developed based on the displacement of Smac 7-mer from BIR3. Through the physical and biochemical analysis of a variety of peptides, we have determined the minimum sequence required for inhibition of the Smac-BIR3 interaction and detailed the dimensions and topology of the BIR3 peptide binding pocket. This work describes the structure-activity relationship (SAR) for peptide inhibitors of Smac-IAP binding.

SUBMITTER: Sharma SK 

PROVIDER: S-EPMC2710984 | biostudies-other | 2006 Mar

REPOSITORIES: biostudies-other

Similar Datasets

| S-EPMC3534930 | biostudies-literature
| S-EPMC6309908 | biostudies-literature
| S-EPMC7739374 | biostudies-literature
| S-EPMC6151827 | biostudies-other
| S-EPMC3252583 | biostudies-literature
| S-EPMC3321198 | biostudies-literature
| S-EPMC6975060 | biostudies-literature
| S-EPMC3139828 | biostudies-other
| S-EPMC2677451 | biostudies-literature
| S-EPMC7553367 | biostudies-literature