Kwon, Hyuk Sung Kim, Da-Rae Yang, Eun Gyeong Park, Yong Keun Ahn, Hee-Chul Min, Sun-Joon Ahn, Dae-Ro 2024-01-20T14:04:13Z 2024-01-20T14:04:13Z 2021-09-04 2012-08-15 0960-894X https://pubs.kist.re.kr/handle/201004/128975 Vascular endothelial growth factor (VEGF) plays a pro-angiogenic role in tumor progression. Stabilization of a key regulator termed the hypoxia inducible factor (HIF)-1 alpha under oxygen deficient environment around tumor is known to elicit expression of VEGF through binding to p300. Thus, inhibition of the HIF-1 alpha-p300 interaction would lead to down-regulation of VEGF expression, thereby providing potential cancer therapeutics. Here, we have screened a chemical library against the interaction of the HIF-1 alpha-derived peptide with p300 employing a fluorescence polarization-based assay. We have identified a compound as the most prominent inhibitor against the protein-protein interaction. Further, we have observed suppression of the mRNA level of VEGF upon treatment of HeLa cells with the compound, demonstrating its inhibitory effect at the cellular level. (c) 2012 Elsevier Ltd. All rights reserved. English Pergamon Press Ltd. CANCER-THERAPY HEPATOMA-CELLS HYPOXIA-INDUCIBLE-FACTOR-1-ALPHA EXPRESSION ACCUMULATION HIF-1-ALPHA CARCINOMA TARGET Inhibition of VEGF transcription through blockade of the hypoxia inducible factor-1 alpha-p300 interaction by a small molecule Article 10.1016/j.bmcl.2012.06.054 1 Bioorganic & Medicinal Chemistry Letters, v.22, no.16, pp.5249 - 5252 Bioorganic & Medicinal Chemistry Letters 22 16 5249 5252 scie scopus 000306962800018 2-s2.0-84864412437 Chemistry, Medicinal Chemistry, Organic Pharmacology & Pharmacy Chemistry Article CANCER-THERAPY HEPATOMA-CELLS HYPOXIA-INDUCIBLE-FACTOR-1-ALPHA EXPRESSION ACCUMULATION HIF-1-ALPHA CARCINOMA TARGET HIF-1 alpha-p300 interaction VEGF Inhibitor Fluorescence polarization Protein-protein interaction