Inhibition of a prolyl hydroxylase domain (PHD) by substrate analog peptides
- Inhibition of a prolyl hydroxylase domain (PHD) by substrate analog peptides
- 권혁성; 최연경; 김정원; 박용근; 양은경; 안대로
- HIF-1α; PHD2; Substrate analog peptides; Peptide inhibitors; Hypoxia
- Issue Date
- Bioorganic & medicinal chemistry letters
- VOL 21, NO 14, 4325-4328
- Oxygen dependent degradation of hypoxia-inducible factor (HIF)-1a 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.
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