Document Report Card
Basic Information
ID: ALA1800070
Journal: Bioorg Med Chem Lett
Title: Inhibition of a prolyl hydroxylase domain (PHD) by substrate analog peptides.
Authors: Kwon HS, Choi YK, Kim JW, Park YK, Yang EG, Ahn DR.
Abstract: Oxygen dependent degradation of hypoxia-inducible factor (HIF)-1α is triggered with hydroxylation by proline hydroxylase domain 2 (PHD2) under normoxic conditions. Some of previously developed PHD2 inhibitors show a considerable potency against factor inhibiting HIF (FIH), the HIF asparagine hydroxylase. For specific inhibition of PHD2, we have synthesized peptides containing 556-575 residues of HIF-1α with modifications at the Pro-564 and examined their inhibitory effect against PHD2. Adopting fluorescence polarization-based assays, we evaluated inhibitory potency of the peptides and selected potent inhibitors. These PHD2 inhibitor peptides showed no significant potency against FIH, demonstrating their specific inhibitory effect on PHD2.
CiteXplore: 21665470