title: 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.affiliation: Auckland Cancer Society Research Centre, School of Medical Sciences, The University of Auckland, Private Bag 92019, Auckland, New Zealand. b.denny@auckland.ac.nz
authors.forename: William A
authors.initials: WA
authors.lastname: Denny
mesh_terms: D000740:Anemia / Q000188:drug therapy*; D000818:Animals; D001372:Aza Compounds / Q000138:chemical synthesis*; D006801:Humans; D006827:Hydantoins / Q000138:chemical synthesis*; D051793:Hypoxia-Inducible Factor 1 / Q000378:metabolism*; D064799:Hypoxia-Inducible Factor-Proline Dioxygenases; D011393:Procollagen-Proline Dioxygenase / Q000037:antagonists & inhibitors*; D013141:Spiro Compounds / Q000138:chemical synthesis*
chemical_list: D001372:Aza Compounds; D006827:Hydantoins; D051793:Hypoxia-Inducible Factor 1; D013141:Spiro Compounds; C490190:EGLN1 protein, human; D011393:Procollagen-Proline Dioxygenase; D064799:Hypoxia-Inducible Factor-Proline Dioxygenases