Nuclear Receptors act as transcription factors that mediate the effects of certain hormones, drugs, and other xenobiotics by modulating the expression of specific genes involved in many cellular fuctions such as development, reproduction, and metabolism. Conserved functional domains of nuclear receptors such as the DNA-binding domain (DBD), ligand-binding domain (LBD), N- and C-terminal transcriptional activation domains, define this class of transcription factors. Their disparate physiologic roles are determined by diversity in both ligand and DNA binding specificties, as well as in specific interactions with co-activator and co-repressor molecules that combinatorially mediate transcription. A major focus in the current discovery of drugs targeting nuclear receptors is identifying drugs with reduced side effects by improving selectivity, not only from other receptors, but also by selective modulation of the nuclear receptor of interest.
Date of publication: 2014
Author: Jack Vanden Heuvel, PhD; INDIGO Biosciences, Inc.