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

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.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Kwon HS,Choi YK,Kim JW,Park YK,Yang EG,Ahn DR

doi

10.1016/j.bmcl.2011.05.050

subject

Has Abstract

pub_date

2011-07-15 00:00:00

pages

4325-8

issue

14

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(11)00679-2

journal_volume

21

pub_type

杂志文章

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