Liver x receptor: a novel therapeutic target

Indian J Pharm Sci. 2008 Mar-Apr;70(2):135-44. doi: 10.4103/0250-474X.41445.


The liver X receptors alpha and beta are orphan nuclear receptors that are key regulators in maintaining cholesterol homeostasis. Originally they were found to play an important role in reverse cholesterol transport, a pathway for the removal of excess cellular cholesterol. However several groups have now shown that the liver X receptors also functions in lipid and carbohydrate metabolism, cellular differentiation, apoptosis and many immune responses. Tissue distribution of the two paralogues differs with liver X receptor beta ubiquitously expressed, while liver X receptor alpha is confined to the liver, kidney, intestine, spleen, adipose tissue, macrophages and skeletal muscle. The endogenous ligands for the liver X receptors are certain oxidized derivatives of cholesterol, the oxysterols. Upon activation by oxysterols, the receptors form obligate heterodimers with retinoid X receptors alpha, beta and gamma; and become competent to activate the transcription of target genes.

Keywords: GLUT1; Liver X Receptors; PPARs; Retinoid X Receptors; SMRT.