A novel fluorescence competition assay for retinoic acid binding proteins

Tomlinson, Charles W.E.; Chisholm, David R.; Valentine, Roy; Whiting, Andrew; Pohl, Ehmke

doi:10.1021/acsmedchemlett.8b00420

A novel fluorescence competition assay for retinoic acid binding proteins

Tomlinson, Charles W.E.; Chisholm, David R.; Valentine, Roy; Whiting, Andrew; Pohl, Ehmke

Authors

Charles W.E. Tomlinson

Dr David Chisholm d.r.chisholm@durham.ac.uk
Academic Visitor

Roy Valentine

Professor Andrew Whiting andy.whiting@durham.ac.uk
Emeritus Professor

Professor Ehmke Pohl ehmke.pohl@durham.ac.uk
Professor

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.

Citation

Tomlinson, C. W., Chisholm, D. R., Valentine, R., Whiting, A., & Pohl, E. (2018). A novel fluorescence competition assay for retinoic acid binding proteins. ACS Medicinal Chemistry Letters, 9(12), 1297–1300-1300. https://doi.org/10.1021/acsmedchemlett.8b00420

Journal Article Type	Article
Acceptance Date	Nov 9, 2018
Online Publication Date	Nov 9, 2018
Publication Date	Dec 31, 2018
Deposit Date	Nov 13, 2018
Publicly Available Date	Nov 9, 2019
Journal	ACS Medicinal Chemistry Letters
Print ISSN	1948-5875
Electronic ISSN	1948-5875
Publisher	American Chemical Society
Peer Reviewed	Peer Reviewed
Volume	9
Issue	12
Pages	1297–1300-1300
DOI	https://doi.org/10.1021/acsmedchemlett.8b00420

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