Sequence-directed recognition peptides: inhibition of endothelin generation via a substrate-depletion mechanism.
Sequence-directed recognition peptides (SDRPs) were constructed on the basis of their hydropathic complementarity for big-endothelin (bigET). These peptides can inhibit in vitro the proteolytic cleavage that generates endothelin (ET) from its bigET precursor. Comparison of dissociation constants of the complexes SDRP:bigET with kinetic constants obtained for the cleavage of bigET by alpha-chymotrypsin (taken as a model proteinase) provides evidence of the potential of SDRPs. This is a novel application of SDRPs used as inhibitors of a proteolytic reaction.
Research Laboratories, Farmitalia-Carlo Erba, Milano, Italy.
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Zamai
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VR
Caiolfa
D000595:Amino Acid Sequence; D002918:Chymotrypsin; D016232:Endothelins / Q000096:biosynthesis / Q000737:chemistry*; D006801:Humans; D007700:Kinetics; D008969:Molecular Sequence Data; D009842:Oligopeptides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D010446:Peptide Fragments / Q000737:chemistry / Q000302:isolation & purification; D011498:Protein Precursors / Q000737:chemistry* / Q000187:drug effects
D016232:Endothelins; D009842:Oligopeptides; D010446:Peptide Fragments; D011498:Protein Precursors; D002918:Chymotrypsin