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A novel fluorescence competition assay for retinoic acid binding proteins.

Tomlinson, Charles W.E. and Chisholm, David R. and Valentine, Roy and Whiting, Andrew and Pohl, Ehmke (2018) 'A novel fluorescence competition assay for retinoic acid binding proteins.', ACS medicinal chemistry letters., 9 (12). 1297–1300-1300.

Abstract

Vitamin A derived retinoid compounds have multiple, powerful roles in the cellular growth and development cycle, and as a result have attracted significant attention from both academic and pharmaceutical research in developing and characterizing synthetic retinoid analogues. Simplifying the hit development workflow for retinoid signaling will improve options available for tackling related pathologies, including tumor growth and neurodegeneration. Here we present a novel assay that employs an intrinsically fluorescent synthetic retinoid, DC271, which allows direct measurement of the binding of non-labeled compounds to relevant proteins. The method allows for straightforward initial measurement of binding using existing compound libraries, and is followed by calculation of binding constants using a dilution series of plausible hits. The ease of use, high throughput format, and measurement of both qualitative and quantitative binding, offer a new direction for retinoid-related pharmacological development.

Item Type:Article
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Status:Peer-reviewed
Publisher Web site:https://doi.org/10.1021/acsmedchemlett.8b00420
Publisher statement:This is an open access article published under a Creative Commons Attribution (CC-BY) License, which permits unrestricted use, distribution and reproduction in any medium, provided the author and source are cited.
Date accepted:09 November 2018
Date deposited:13 November 2018
Date of first online publication:09 November 2018
Date first made open access:09 November 2019

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