Conformationally Constrained Inhibitors Of Caspase-1 (Interleukin-1 Beta Converting Enzyme) And Of The Human Ced-3 Homologue Caspase-3 (Cpp32, Apopain)

A systematic study of interleukin-lp converting enzyme (ICE, caspase-1) and caspase-3 (CPP32, apopain) inhibitors incorporating a PGammaP3 conformationally constrained dipeptide mimetic is reported. Depending on the nature of the P-4 substituent, highly selective inhibitors of both Csp-l or Csp-3 were obtained. (C) 1998 Elsevier Science Ltd. All rights reserved.