[Organophosphate analogs of biologically active compounds. XIV. Halophosphonate analogs of ATP as acetyl CoA carboxylase inhibitors]

Bioorg Khim. 1985 May;11(5):598-604.
[Article in Russian]

Abstract

Halophosphonate ATP analogues pp[CHBr]pA and p[CHBr]ppA synthesised from bromomethylenebisphosphonate and adenosine derivatives, proved to be effective competitive inhibitors of Ac-CoA-carboxylase (CE 6.4.1.2) from rat liver (Ki = 0,2 mM). The inhibitory effects of both analogues were reversible and higher than those of some other ATP analogues. Another enzyme, Ac-CoA-synthetase (CE 6.2.1.1), with a different mode of ATP-cleavage showed wider specificity to ATP-analogues than Ac-CoA-carboxylase.

Publication types

  • English Abstract

MeSH terms

  • Acetate-CoA Ligase / antagonists & inhibitors*
  • Acetyl-CoA Carboxylase / antagonists & inhibitors*
  • Adenosine
  • Adenosine Triphosphate / analogs & derivatives
  • Animals
  • Chemical Phenomena
  • Chemistry
  • Coenzyme A Ligases / antagonists & inhibitors*
  • Cytosol / enzymology
  • Diphosphonates
  • In Vitro Techniques
  • Ligases / antagonists & inhibitors*
  • Liver / enzymology
  • Myocardium / ultrastructure
  • Rabbits
  • Rats

Substances

  • 5'-adenylyl (beta,gamma-bromomethylene)diphosphonate
  • Diphosphonates
  • bromomethylenebis(phosphonic acid)
  • Adenosine Triphosphate
  • 5'-adenylyl (alpha,beta-bromomethylene)diphosphonate
  • Ligases
  • Coenzyme A Ligases
  • Acetate-CoA Ligase
  • Acetyl-CoA Carboxylase
  • Adenosine