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Identification of potent and novel small-molecule inhibitors of caspase-3

Darin A Allen1, Phuongly Pham, Ingrid C Choong

  • 1Sunesis Pharmaceuticals, Inc., 341 Oyster Point Boulevard, South San Francisco, CA 94080, USA. dallen@sunesis.com

Bioorganic & Medicinal Chemistry Letters
|October 14, 2003
PubMed

Abstract:

The design and synthesis of a series of novel, reversible, small molecule inhibitors of caspase-3 are described.

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Caspases01:24

Caspases

Caspase, a family of cysteine proteases, serve as effectors in apoptosis. The ced3 gene in C.elegans was first identified to be involved in apoptosis. This gene encodes the ced-3 caspase that is similar to the interleukin-1-beta converting enzyme or ICE in mammals. In addition to apoptosis, caspases also function in the inflammatory response. Inflammatory caspases are essential in activating pro-inflammatory cytokines that recruit immune cells and block the replication of pathogens inside cells.

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