Download MendeleyBenzimidazole-2-pyrazole HIF Prolyl 4-Hydroxylase Inhibitors as Oral Erythropoietin Secretagogues.
Rosen, M.D., Venkatesan, H., Peltier, H.M., Bembenek, S.D., Kanelakis, K.C., Zhao, L.X., Leonard, B.E., Hocutt, F.M., Wu, X., Palomino, H.L., Brondstetter, T.I., Haugh, P.V., Cagnon, L., Yan, W., Liotta, L.A., Young, A., Mirzadegan, T., Shankley, N.P., Barrett, T.D., Rabinowitz, M.H.(2010) ACS Med Chem Lett 1: 526-529
- PubMed: 24900242
- DOI: https://doi.org/10.1021/ml100198y
- Primary Citation of Related Structures:
3OUH, 3OUI, 3OUJ - PubMed Abstract:
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.
Organizational Affiliation:
Johnson & Johnson Pharmaceutical Research and Development, L.L.C, 3210 Merryfield Row, San Diego, California 92121, United States.
