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A novel fluorescence competition assay for retinoic acid binding proteins

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

A novel fluorescence competition assay for retinoic acid binding proteins Thumbnail


Authors

Charles W.E. Tomlinson

Roy Valentine



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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Copyright 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.







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