Princeton University

Yigong Shi

Martin F Semmelhack

George McLendon

Martin Case

Philip A Albiniak

Rachael A Kipp

Aislyn D Wist

Compounds that bind cellular IAPs (inhibitor of apoptosis proteins) are disclosed. The compounds are mimetics of the N-terminal tetrapeptide of IAP-binding proteins, such as Smac/DIABOLO, IIid, Grim and Reaper, which interact with a specific surface groove of IAP. Also disclosed are methods of using these compounds for therapeutic, diagnostic and assay purposes.

IAP binding compounds

The structure of a soluble, functional fragment of human Apaf-1 protein having ADP bound thereto is disclosed. The invention includes such soluble, functional fragments of human Apaf-1 and other metazoan Apaf-1 homologs. Also included in the invention are methods of making such fragments and methods of using them, for example in screening methods to identify adenine nucleotide analogs and other compounds useful for alleviating or preventing disease conditions associated with inappropriate regulation of apoptosis.

Soluble, functional apoptotic protease-activating factor 1 fragments

Peptides and peptidomimetics capable of modulating apoptosis through their interaction with cellular IAPs (inhibitor of apoptosis proteins) are disclosed. The peptides and mimetics are based on the N-terminal tetrapeptide of IAP-binding proteins, such as Smac/DIABLO, Hid, Grim and Reaper, which interact with a specific surface groove of IAP. Also disclosed are methods of using these peptides and peptidomimetics for therapeutic purposes and for rational drug design.

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Plainsboro, NJ, United States of America

Yigong Shi