Vitamin K-dependent carboxylase: synthesis of an inhibitor of the glutamyl binding site

FEBS Lett. 1983 Feb 7;152(1):79-82. doi: 10.1016/0014-5793(83)80486-4.

Abstract

Liver microsomes contain a vitamin K and O2-dependent carboxylase that converts peptide-bound glutamyl residues to gamma-carboxyglutamate residues. The peptide Boc-O-phospho-Ser-O-phospho-Ser-Leu-OMe has now been synthesized. This peptide inhibits the carboxylation of endogenous protein precursors by a detergent-solubilized preparation of the carboxylase and is an apparent competitive inhibitor of the carboxylation of Phe-Leu-Glu-Glu-Leu.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • 1-Carboxyglutamic Acid / biosynthesis
  • Amino Acid Sequence
  • Animals
  • Carbon-Carbon Ligases*
  • Kinetics
  • Ligases / antagonists & inhibitors*
  • Microsomes, Liver / enzymology*
  • Oligopeptides / chemical synthesis
  • Peptide Fragments / pharmacology
  • Rats
  • Structure-Activity Relationship
  • Vitamin K / metabolism*

Substances

  • Oligopeptides
  • Peptide Fragments
  • Vitamin K
  • 1-Carboxyglutamic Acid
  • Ligases
  • Carbon-Carbon Ligases
  • glutamyl carboxylase