Target intelligence / Profile preview

Liver X receptor (LXR)

Target
LXR
Molecular classification
Nuclear receptor, Transcription factor
01

Overview

Liver X receptors (LXRs) are nuclear receptors that play a central role in regulating cholesterol, fatty acid, and glucose homeostasis. They function as transcription factors activated by endogenous ligands—primarily oxysterols, which are oxidized derivatives of cholesterol. LXRs act as cellular cholesterol sensors and are considered promising targets for treating metabolic disorders. Activation may also promote hepatic steatosis/hypertriglyceridemia due to increased lipogenesis.

02

Mechanism of action

Upon binding their ligands, LXRs form heterodimers with RXR isoforms. These complexes bind to liver X response elements in target gene promoters to regulate transcription, modulating genes involved in cholesterol, fatty acid, and glucose homeostasis, as well as inflammation.

03

Biological functions

Cholesterol homeostasisLipid metabolismGlucose metabolismImmune regulationInflammation controlCell differentiationApoptosisAdrenal steroid synthesisSkin aging processesMale fertility regulation
04

Disease associations

AtherosclerosisDiabetesNeurodegenerative diseases
05

Safety considerations

Hepatic steatosisHypertriglyceridemia
06

Interacting drugs

Oxysterols

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