sr9009 and Immune-System-Diseases

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.

Topics: Animals; Circadian Rhythm; Heme; Humans; Immune System Diseases; Ligands; Nuclear Receptor Subfamily 1, Group D, Member 1; Receptors, Cytoplasmic and Nuclear; Repressor Proteins; Structure-Activity Relationship