Kwon, Hyuk Sung Choi, Yien Kyoung Kim, Jeong Won Park, Yong Keun Yang, Eun Gyeong Ahn, Dae-Ro 2024-01-20T16:34:18Z 2024-01-20T16:34:18Z 2021-09-05 2011-07-15 0960-894X https://pubs.kist.re.kr/handle/201004/130180 Oxygen dependent degradation of hypoxia-inducible factor (HIF)-1 alpha 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-1 alpha 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. (C) 2011 Elsevier Ltd. All rights reserved. English Pergamon Press Ltd. HIF HIF-1-ALPHA REVEALS Inhibition of a prolyl hydroxylase domain (PHD) by substrate analog peptides Article 10.1016/j.bmcl.2011.05.050 1 Bioorganic & Medicinal Chemistry Letters, v.21, no.14, pp.4325 - 4328 Bioorganic & Medicinal Chemistry Letters 21 14 4325 4328 scie scopus 000292186400045 2-s2.0-79959869553 Chemistry, Medicinal Chemistry, Organic Pharmacology & Pharmacy Chemistry Article HIF HIF-1-ALPHA REVEALS HIF-1 alpha PHD2 Substrate analog peptides Peptide inhibitors Hypoxia