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

Moreno Zamai, Valeria R. Caiolfa

Research output: Contribution to journalArticle

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 languageEnglish
Pages (from-to)337-340
Number of pages4
JournalBiochimica et Biophysica Acta (BBA)/Protein Structure and Molecular
Volume1202
Issue number2
DOIs
Publication statusPublished - Oct 6 1993

Fingerprint

Endothelins
Endothelin-1
Peptides
Substrates
Chymotrypsin
Peptide Hydrolases
Kinetics

Keywords

  • big-Endothelin
  • Complementary peptide
  • Endothelin biosynthesis
  • Substrate depletion

ASJC Scopus subject areas

  • Biochemistry
  • Biophysics
  • Molecular Biology
  • Structural Biology
  • Medicine(all)

Cite this

@article{2815f38abc744fb38885718081486f92,
title = "Sequence-directed recognition peptides: inhibition of endothelin generation via a substrate-depletion mechanism",
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.",
keywords = "big-Endothelin, Complementary peptide, Endothelin biosynthesis, Substrate depletion",
author = "Moreno Zamai and Caiolfa, {Valeria R.}",
year = "1993",
month = "10",
day = "6",
doi = "10.1016/0167-4838(93)90025-M",
language = "English",
volume = "1202",
pages = "337--340",
journal = "Biochimica et Biophysica Acta - Protein Structure and Molecular Enzymology",
issn = "0167-4838",
publisher = "Elsevier BV",
number = "2",

}

TY - JOUR

T1 - Sequence-directed recognition peptides

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

AU - Zamai, Moreno

AU - Caiolfa, Valeria R.

PY - 1993/10/6

Y1 - 1993/10/6

N2 - 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.

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

UR - http://www.scopus.com/inward/record.url?scp=0027910612&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=0027910612&partnerID=8YFLogxK

U2 - 10.1016/0167-4838(93)90025-M

DO - 10.1016/0167-4838(93)90025-M

M3 - Article

C2 - 8399398

AN - SCOPUS:0027910612

VL - 1202

SP - 337

EP - 340

JO - Biochimica et Biophysica Acta - Protein Structure and Molecular Enzymology

JF - Biochimica et Biophysica Acta - Protein Structure and Molecular Enzymology

SN - 0167-4838

IS - 2

ER -