Journal
ACS MEDICINAL CHEMISTRY LETTERS
Volume 1, Issue 9, Pages 526-529Publisher
AMER CHEMICAL SOC
DOI: 10.1021/ml100198y
Keywords
Prolyl 4-hydroxylase inhibitors; PHD inhibitors; hypoxia inducible factor; HIF; erythropoietin; epo; erythropoietin stimulating agents; anemia
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HIF prolyl 4-hydroxylases (PHD) are a family of enzymes that mediate key physiological responses to hypoxia by modulating the levels of hypoxia inducible factor 1-alpha (HIF1 alpha). Certain benzimidazole-2-pyrazole carboxylates were discovered to be PHD2 inhibitors using ligand- and structure-based methods and found to be potent, orally efficacious stimulators of erythropoietin secretion in vivo.
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