[Synthesis and biological activity of analogs of a nonapeptide inhibitor of peptidyldipeptidase]

M P Filatova; N A Krit; N V Beschastnaia; A V Blokhina; N I Kozlova

[Synthesis and biological activity of analogs of a nonapeptide inhibitor of peptidyldipeptidase]

Bioorg Khim. 1985 Jan;11(1):21-30.

[Article in Russian]

Authors

M P Filatova, N A Krit, N V Beschastnaia, A V Blokhina, N I Kozlova

PMID: 2985089

Abstract

The synthesis of 5 analogues of the effective inhibitor of peptidyl dipeptidase, teprotide, has been carried out. The inhibitory and bradykinin-potentiating activity of these compounds has been assayed. N-Terminal pyroglutamic acid and positive charge of arginine in position 4 were found to be essential for biological activity of the inhibitor.

Publication types

English Abstract

MeSH terms

Amino Acid Sequence
Angiotensin-Converting Enzyme Inhibitors*
Animals
Bradykinin / pharmacology
Chemical Phenomena
Chemistry
Circular Dichroism
Drug Synergism
Guinea Pigs
Ileum / drug effects
In Vitro Techniques
Muscle Contraction / drug effects
Muscle, Smooth / drug effects
Oligopeptides / chemical synthesis*
Protein Conformation
Teprotide / analogs & derivatives
Teprotide / chemical synthesis*
Teprotide / pharmacology

Substances

Angiotensin-Converting Enzyme Inhibitors
Oligopeptides
Teprotide
Bradykinin