2-Oxoglutarate analogue inhibitors of prolyl hydroxylase domain 2

Bioorg Med Chem Lett. 2009 Nov 1;19(21):6192-5. doi: 10.1016/j.bmcl.2009.09.005. Epub 2009 Sep 6.

Abstract

Analogues of the 2-oxoglutarate cosubstrate of the human oxygen sensing enzyme prolyl hydroxylase domain 2 (PHD2) with variations in the potential iron-chelating group were screened as inhibitors and for binding (using non-denaturing electrospray ionization mass spectrometry) to PHD2.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Fluorescence Resonance Energy Transfer
  • Humans
  • Iron Chelating Agents
  • Ketoglutaric Acids / chemistry*
  • Ketoglutaric Acids / pharmacology
  • Procollagen-Proline Dioxygenase / antagonists & inhibitors*
  • Procollagen-Proline Dioxygenase / metabolism
  • Protein Binding
  • Protein Structure, Tertiary
  • Spectrometry, Mass, Electrospray Ionization

Substances

  • Iron Chelating Agents
  • Ketoglutaric Acids
  • Procollagen-Proline Dioxygenase