NR1H3

NR1H3 encodes Liver X Receptor Alpha (LXRα), a nuclear receptor also known as LXRa, RLD-1, or NER. It forms functional heterodimers with retinoid X receptor (RXR) and binds to LXR response elements (LXREs) in target gene promoters. LXRα regulates lipid homeostasis—promoting cholesterol reverse transport via ABCA1/ABCG1 and modulating hepatic fatty acid synthesis.
Dysregulation of NR1H3 is linked to atherosclerosis (impaired cholesterol clearance) and non-alcoholic fatty liver disease (NAFLD). Synthetic agonists like T0901317 show preclinical efficacy but induce hypertriglyceridemia. Current research focuses on tissue-specific agonists to mitigate side effects, though no LXRα-targeted drugs are clinically approved yet.