High-quality crystals of human haematopoietic prostaglandin D synthase with novel inhibitors

Acta Crystallogr Sect F Struct Biol Cryst Commun. 2010 Jul 1;66(Pt 7):846-50. doi: 10.1107/S1744309110020828. Epub 2010 Jun 24.

Abstract

Human haematopoietic prostaglandin D synthase (H-PGDS; EC 5.3.99.2) produces prostaglandin D(2), an allergic and inflammatory mediator, in mast cells and Th2 cells. H-PGDS has been crystallized with novel inhibitors with half-maximal inhibitory concentrations (IC(50)) in the low nanomolar range by the counter-diffusion method onboard the Russian Service Module on the International Space Station. The X-ray diffraction of a microgravity-grown crystal of H-PGDS complexed with an inhibitor with an IC(50) value of 50 nM extended to 1.1 A resolution at 100 K using SPring-8 synchrotron radiation, which is one of the highest resolutions obtained to date for this protein.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Crystallization
  • Crystallography, X-Ray
  • Enzyme Inhibitors / chemistry*
  • Humans
  • Intramolecular Oxidoreductases / antagonists & inhibitors
  • Intramolecular Oxidoreductases / chemistry*
  • Lipocalins / antagonists & inhibitors
  • Lipocalins / chemistry*

Substances

  • Enzyme Inhibitors
  • Lipocalins
  • Intramolecular Oxidoreductases
  • prostaglandin R2 D-isomerase