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. 1998 Oct 6;8(19):2757-62.
doi: 10.1016/s0960-894x(98)00498-3.

Conformationally constrained inhibitors of caspase-1 (interleukin-1 beta converting enzyme) and of the human CED-3 homologue caspase-3 (CPP32, apopain)

D S Karanewsky  1 , X Bai, S D Linton, J F Krebs, J Wu, B Pham, K J Tomaselli
Affiliations

Conformationally constrained inhibitors of caspase-1 (interleukin-1 beta converting enzyme) and of the human CED-3 homologue caspase-3 (CPP32, apopain)

D S Karanewsky et al. Bioorg Med Chem Lett. .

Abstract

A systematic study of interleukin-1 beta converting enzyme (ICE, caspase-1) and caspase-3 (CPP32, apopain) inhibitors incorporating a P2-P3 conformationally constrained dipeptide mimetic is reported. Depending on the nature of the P4 substituent, highly selective inhibitors of both Csp-1 or Csp-3 were obtained.

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