The development of methodologies for high-throughput retinoic acid binding assays in drug discovery and beyond

Assays for identifying the activity of retinoic acids and retinoic acid derivatives, have become increasingly accessible in the 21st century. Movement away from complex in cellulo expression and radiological systems toward accessible FRET or fluorescent compound led studies has increased the accessi...

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Veröffentlicht in:Methods in enzymology 2020, Vol.637, p.539-560
Hauptverfasser: Tomlinson, Charles W E, Whiting, Andrew
Format: Artikel
Sprache:eng
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Zusammenfassung:Assays for identifying the activity of retinoic acids and retinoic acid derivatives, have become increasingly accessible in the 21st century. Movement away from complex in cellulo expression and radiological systems toward accessible FRET or fluorescent compound led studies has increased the accessibility and high-throughput capabilities of the field. The improvement in assaying technologies will lead to both increased and faster screening of retinoids and related compounds, improving drug discovery workflows and implementation pipelines. This enabling technology will allow better understanding of the huge range of phenotypes closely linked to retinoid signaling, and through the development of improved treatments improve outlooks for diagnoses in these cases and those of closely related diseases. In this chapter we present an examination of historical and modern techniques for assaying the activity of retinoic acid derivatives against their binding proteins.
ISSN:1557-7988
DOI:10.1016/bs.mie.2020.02.008