Target Validation Information
TTD ID	T53904
Target Name	HIF-prolyl hydroxylase 1 (HPH-1)
Type of Target	Successful
Drug Potency against Target	2-(carboxymethylamino)-2-oxoacetic acid	Drug Info	IC50 = 2100 nM	[1]
	Pyridine-2,4-dicarboxylic acid	Drug Info	IC50 = 1500 nM	[1]
Action against Disease Model	FG-4592	Drug Info	Preclinical data were reported demonstrating several novel and beneficial pharmacodynamic effects resulting from 'complete erythropoiesis' induced by HIF-PHI FG-2216 and FG-4592including coordinate regulation of genes that mediate erythropoiesis leading to production of EPO by cells in the kidney and liver; mobilization and proper utilization of iron stores; and erythropoiesis despite interference from chronic inflammation. The latter effect was demonstrated in a model of anemia of chronic disease and is consistent with previously reported data showing that HIF-PHI can suppress inflammatory pathways, such as IL-12-mediated T helper cell production of pro-inflammatory cytokines (e.g., TNF-alpha and IFN-gamma) and down-regulate hepcidin, a regulatory hormone that limits iron availability and thus suppresses erythropoiesis under conditions of inflammation
References
REF 1	Design, synthesis, enzyme-inhibitory activity, and effect on human cancer cells of a novel series of jumonji domain-containing protein 2 histone de... J Med Chem. 2010 Aug 12;53(15):5629-38.

If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.