Inhibition of VEGF transcription through blockade of the hypoxia inducible factor-1α-p300 interaction by a small molecule

Title
Inhibition of VEGF transcription through blockade of the hypoxia inducible factor-1α-p300 interaction by a small molecule
Authors
권혁성김다래양은경박용근안희철민선준안대로
Keywords
HIF-1α?p300 interaction; VEGF; Inhibitor; Fluorescence polarization; Protein?protein interaction
Issue Date
2012-08
Publisher
Bioorganic & medicinal chemistry letters
Citation
VOL 22, NO 16, 5249-5252
Abstract
Vascular endothelial growth factor (VEGF) plays a pro-angiogenic role in tumor progression. Stabilization of a key regulator termed the hypoxia inducible factor (HIF)-1α under oxygen deficient environment around tumor is known to elicit expression of VEGF through binding to p300. Thus, inhibition of the HIF-1α–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-1aderived 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.
URI
http://pubs.kist.re.kr/handle/201004/43980
ISSN
0960894X
Appears in Collections:
KIST Publication > Article
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