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.
Keywords:
Drug development; REV-ERB; Transcription factor.
Copyright © 2020 Elsevier Ltd. All rights reserved.
Publication types
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Research Support, Non-U.S. Gov't
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Review
MeSH terms
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Animals
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Circadian Rhythm / physiology
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Heme / chemistry
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Humans
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Immune System Diseases / metabolism
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Immune System Diseases / pathology
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Ligands
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Nuclear Receptor Subfamily 1, Group D, Member 1 / agonists
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Nuclear Receptor Subfamily 1, Group D, Member 1 / antagonists & inhibitors
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Nuclear Receptor Subfamily 1, Group D, Member 1 / metabolism
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Receptors, Cytoplasmic and Nuclear / agonists
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Receptors, Cytoplasmic and Nuclear / antagonists & inhibitors
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Receptors, Cytoplasmic and Nuclear / metabolism*
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Repressor Proteins / agonists
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Repressor Proteins / antagonists & inhibitors
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Repressor Proteins / metabolism
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Structure-Activity Relationship
Substances
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Ligands
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NR1D1 protein, human
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NR1D2 protein, human
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Nuclear Receptor Subfamily 1, Group D, Member 1
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Receptors, Cytoplasmic and Nuclear
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Repressor Proteins
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Heme