Inhibition of a prolyl hydroxylase domain (PHD) by substrate analog peptides

Title
Inhibition of a prolyl hydroxylase domain (PHD) by substrate analog peptides
Authors
권혁성최연경김정원박용근양은경안대로
Keywords
HIF-1α; PHD2; Substrate analog peptides; Peptide inhibitors; Hypoxia
Issue Date
2011-07
Publisher
Bioorganic & medicinal chemistry letters
Citation
VOL 21, NO 14, 4325-4328
Abstract
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.
URI
http://pubs.kist.re.kr/handle/201004/41185
ISSN
0960-894X
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KIST Publication > Article
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