The transcriptional repressor REV-ERB as a novel target for disease
File(s)
Accepted version
Author(s)
Type
Journal Article
Abstract
REV-ERB is a member of the nuclear receptor superfamily of transcription factors involved in the regulation of many physiological processes, from circadian rhythm, to immune function and metabolism. Accordingly, REV-ERB has been considered as a promising, but difficult drug target for the treatment of numerous diseases. Here, we concisely review current understanding of the function of REV-ERB, modulation by endogenous factors and synthetic ligands, and the involvement of REV-ERB in select human diseases. Particular focus is placed on the medicinal chemistry of synthetic REV-ERB ligands, which demonstrates the need for higher quality ligands to aid in robust validation of this exciting target.
Date Issued
2020-09-01
Date Acceptance
2020-07-04
Citation
Bioorganic & Medicinal Chemistry Letters, 2020, 30 (17), pp.127395-127395
ISSN
0960-894X
Publisher
Elsevier BV
Start Page
127395
End Page
127395
Journal / Book Title
Bioorganic & Medicinal Chemistry Letters
Volume
30
Issue
17
Copyright Statement
© 2020 Elsevier Ltd. All rights reserved. This manuscript is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 4.0 International Licence http://creativecommons.org/licenses/by-nc-nd/4.0/
Sponsor
Cancer Research UK
Engineering & Physical Science Research Council (EPSRC)
Identifier
https://www.sciencedirect.com/science/article/pii/S0960894X20305060?via%3Dihub
Grant Number
23619
EP/R00188X/1
Subjects
Medicinal & Biomolecular Chemistry
0304 Medicinal and Biomolecular Chemistry
0305 Organic Chemistry
1115 Pharmacology and Pharmaceutical Sciences
Publication Status
Published online
Article Number
127395
Date Publish Online
2020-07-10