Analogues of dealanylalahopcin are inhibitors of human HIF prolyl hydroxylases

Bioorg Med Chem Lett. 2003 Apr 17;13(8):1451-4. doi: 10.1016/s0960-894x(03)00149-5.

Abstract

Analogues of the naturally occurring cyclic hydroxamate dealanylalahopcin, which is an inhibitor of procollagen prolyl-4-hydroxylase, were synthesised and shown to be inhibitors of the human hypoxia-inducible factor prolyl hydroxylases.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Aminobutyrates / chemical synthesis
  • Aminobutyrates / chemistry*
  • Aminobutyrates / metabolism
  • Aminobutyrates / pharmacology*
  • Animals
  • Autoradiography
  • Binding Sites
  • Enzyme Inhibitors / chemistry
  • Enzyme Inhibitors / pharmacology
  • Humans
  • Hypoxia-Inducible Factor 1, alpha Subunit
  • Iron / metabolism
  • Isoenzymes / antagonists & inhibitors
  • Isoenzymes / metabolism
  • Procollagen-Proline Dioxygenase / antagonists & inhibitors*
  • Procollagen-Proline Dioxygenase / metabolism
  • Transcription Factors / metabolism*
  • Tumor Suppressor Proteins / analysis
  • Tumor Suppressor Proteins / metabolism

Substances

  • Aminobutyrates
  • Enzyme Inhibitors
  • HIF1A protein, human
  • Hypoxia-Inducible Factor 1, alpha Subunit
  • Isoenzymes
  • Transcription Factors
  • Tumor Suppressor Proteins
  • dealanylalahopcin
  • Iron
  • Procollagen-Proline Dioxygenase