Vol. 7, Issue 1, Part D (2025)

As nuclear receptors that control immunological responses, inflammation, and lipid metabolism, liver X receptors (LXRs) are essential modulators of metabolic balance. There are two different isoforms of LXR: LXRα and LXRβ. LXRα primarily affects the balance of cholesterol in the liver, while LXRβ has a more general regulatory role in a variety of tissues. The transcriptional alterations that LXRs cause upon activation by endogenous oxysterols or synthetic ligands control glucose homeostasis, bile acid synthesis, and cholesterol efflux, making them desirable therapeutic targets for atherosclerosis, metabolic disorders, neurodegenerative diseases, and cancer. Despite its potential, off-target effects, metabolic imbalances, and tissue-specific adverse responses make practical translation of LXR modulators difficult. Structural biology, ligand design, and drug delivery system developments are improving methods for creating selective modulators with better safety and effectiveness profiles. The molecular processes, functional dynamics, and therapeutic implications of LXRs are examined in this review, with a focus on new developments that go beyond pharmacological constraints. Research is being conducted to maximize the therapeutic potential of LXRs while reducing undesirable side effects, opening the door for next-generation treatments in inflammatory and metabolic disorders. This is being done by combining insights from precision medicine and omics technology.