A fluorescence polarization assay for identifying ligands that bind to vascular endothelial growth factor.

Analytical Biochemistry
Kimberly J PetersonSamuel H Gellman

Abstract

Vascular endothelial growth factor (VEGF) is a homodimeric proangiogenic protein that induces endothelial cell migration and proliferation primarily through interactions with its major receptors, VEGFR-1 and VEGFR-2. Inhibitors of one or both of these VEGF-receptor interactions could be beneficial as therapeutics for diseases caused by dysfunctional angiogenesis (e.g., cancer). Others have reported small peptides that bind to the VEGF dimer at surface regions that are recognized by the receptors. Here we report the development of a fluorescence polarization assay based on the binding to VEGF of a derivative of one of these peptides that has been labeled with BODIPY-tetramethylrhodamine (BODIPY(TMR)). This 384-well format assay is tolerant to dimethyl sulfoxide (DMSO, up to 4% [v/v]) and has a Z' factor of 0.76, making it useful for identifying molecules that associate with the receptor-binding surface of the VEGF dimer.

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Citations

Apr 28, 2012·Bioconjugate Chemistry·Bernadette V MarquezClaude F Meares
Mar 18, 2010·Chemical Reviews·David M Jameson, Justin A Ross
May 3, 2012·Journal of the American Chemical Society·Holly S HaaseSamuel H Gellman
Apr 1, 2015·Proceedings of the National Academy of Sciences of the United States of America·James W CheccoSamuel H Gellman
Nov 30, 2016·Chembiochem : a European Journal of Chemical Biology·James W Checco, Samuel H Gellman
Jul 31, 2020·Biosensors & Bioelectronics·Ujwal PatilRichard C Willson
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Apr 12, 2018·ACS Chemical Biology·Vladimir S BorodkinDaan M F van Aalten

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