Sequence-directed recognition peptides: inhibition of endothelin generation via a substrate-depletion mechanism

Moreno Zamai; Valeria R. Caiolfa

doi:10.1016/0167-4838(93)90025-M

Sequence-directed recognition peptides: inhibition of endothelin generation via a substrate-depletion mechanism

Moreno Zamai, Valeria R. Caiolfa

IRCCS Ospedale San Raffaele

Research output: Contribution to journal › Article › peer-review

Abstract

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 α-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.

Original language	English
Pages (from-to)	337-340
Number of pages	4
Journal	Biochimica et Biophysica Acta (BBA)/Protein Structure and Molecular
Volume	1202
Issue number	2
DOIs	https://doi.org/10.1016/0167-4838(93)90025-M
Publication status	Published - Oct 6 1993

Keywords

big-Endothelin
Complementary peptide
Endothelin biosynthesis
Substrate depletion

ASJC Scopus subject areas

Biochemistry
Biophysics
Molecular Biology
Structural Biology
Medicine(all)

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10.1016/0167-4838(93)90025-M

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abstract = "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 α-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.",

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T2 - inhibition of endothelin generation via a substrate-depletion mechanism

AU - Zamai, Moreno

AU - Caiolfa, Valeria R.

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AB - 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 α-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.

KW - big-Endothelin

KW - Complementary peptide

KW - Endothelin biosynthesis

KW - Substrate depletion

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Sequence-directed recognition peptides: inhibition of endothelin generation via a substrate-depletion mechanism

Abstract

Keywords

ASJC Scopus subject areas

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