Inhibition of VEGF transcription through blockade of the hypoxia inducible factor-1α-p300 interaction by a small molecule
- Inhibition of VEGF transcription through blockade of the hypoxia inducible factor-1α-p300 interaction by a small molecule
- 권혁성; 김다래; 양은경; 박용근; 안희철; 민선준; 안대로
- HIF-1α?p300 interaction; VEGF; Inhibitor; Fluorescence polarization; Protein?protein interaction
- Issue Date
- Bioorganic & medicinal chemistry letters
- VOL 22, NO 16, 5249-5252
- 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.
- Appears in Collections:
- KIST Publication > Article
- Files in This Item:
There are no files associated with this item.
- RIS (EndNote)
- XLS (Excel)
Items in DSpace are protected by copyright, with all rights reserved, unless otherwise indicated.