Benzimidazole-2-pyrazole HIF Prolyl 4-Hydroxylase Inhibitors as Oral Erythropoietin Secretagogues

Benzimidazole-2-pyrazole HIF Prolyl 4-Hydroxylase Inhibitors as Oral Erythropoietin Secretagogues

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-α (HIF1α). Certain benzimidazole-2-pyrazole carboxylates were discovered to be PHD2 inhibitors using ligand- and structure-based methods...

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Veröffentlicht in:ACS medicinal chemistry letters 2010-12, Vol.1 (9), p.526-529
Hauptverfasser: Rosen, Mark D, Venkatesan, Hariharan, Peltier, Hillary M, Bembenek, Scott D, Kanelakis, Kimon C, Zhao, Lucy X, Leonard, Barry E, Hocutt, Frances M, Wu, Xiaodong, Palomino, Heather L, Brondstetter, Theresa I, Haugh, Peter V, Cagnon, Laurence, Yan, Wen, Liotta, Lisa A, Young, Andrew, Mirzadegan, Tara, Shankley, Nigel P, Barrett, Terrance D, Rabinowitz, Michael H
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Sprache:eng
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Zusammenfassung: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-α (HIF1α). 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.
ISSN:1948-5875
1948-5875
DOI:10.1021/ml100198y