Skip to main content
. Author manuscript; available in PMC: 2015 Dec 1.
Published in final edited form as: Curr Opin Pharmacol. 2014 Oct 6;0:112–119. doi: 10.1016/j.coph.2014.09.013

Figure 1. The multiple mechanisms of nuclear receptor mediated modulation of responsive gene transcription.

Figure 1

Binding of ligand induces a conformational change of the NR that allows receptor dimerization, association with hormone responsive elements (HRE) in the promoters of responsive genes, and recruitment of (A) co-activators resulting in an increase in responsive gene expression, or (B) recruitment of co-repressors that repress gene expression. (C) Nuclear receptor activity can also be induced by receptor phosphorylation of the Activator Function 1 (AF1) domain resulting in ligand independent constitutive activity. (D) Binding of ligand may cause a conformational change of constitutively active or constitutively bound NR that counteracts the effects of a constitutively active receptor. Pharmacologically, such effects are equivalent to inverse-agonist effects.