Giving anemia a boost with inhibitors of prolyl hydroxylase.

Abstract

There is much current interest in the development of inhibitors of the prolyl hydroxylase (PHD) enzymes that regulate the hypoxia-inducible transcription factor (HIF), which in turn stimulates the production of erythropoietin and ultimately red blood cells, as a treatment for anemia. A recent paper reports the synthesis and evaluation of a novel class of potent spirohydantoin-based pan-PHD inhibitors for this purpose. The paper is an exemplar of drug development from high-throughput screen to clinical candidate.

• Authors: William A Denny
• Journal: Journal of medicinal chemistry (J Med Chem) Vol. 55 Issue 7 Pg. 2943-4 (Apr 12 2012) ISSN: 1520-4804 [Electronic] United States
• PMID: 22409479 (Publication Type: Journal Article, Comment)
• Copyright: © 2012 American Chemical Society

Chemical References

• Aza Compounds
• Hydantoins
• Hypoxia-Inducible Factor 1
• Spiro Compounds
• EGLN1 protein, human
• Procollagen-Proline Dioxygenase
• Hypoxia-Inducible Factor-Proline Dioxygenases

Topics

• Anemia (drug therapy)
• Animals
• Aza Compounds (chemical synthesis)
• Humans
• Hydantoins (chemical synthesis)
• Hypoxia-Inducible Factor 1 (metabolism)
• Hypoxia-Inducible Factor-Proline Dioxygenases
• Procollagen-Proline Dioxygenase (antagonists & inhibitors)
• Spiro Compounds (chemical synthesis)