Ligands of Therapeutic Utility for the Liver X Receptors.

Funding Source

National Institute on Minority Health and Health Disparities, National Institutes of Health, National Science Foundation

Grant Number

2G12MD007595, P20GM103424, 1R15GM113193-01,5R25GM060926-10,5RL5GM118966-03, HRD-1505219


Department of Chemistry

Document Type


Publication Date



Liver X receptors (LXRs) have been increasingly recognized as a potential therapeutic target to treat pathological conditions ranging from vascular and metabolic diseases, neurological degeneration, to cancers that are driven by lipid metabolism. Amidst intensifying efforts to discover ligands that act through LXRs to achieve the sought-After pharmacological outcomes, several lead compounds are already being tested in clinical trials for a variety of disease interventions. While more potent and selective LXR ligands continue to emerge from screening of small molecule libraries, rational design, and empirical medicinal chemistry approaches, challenges remain in minimizing undesirable effects of LXR activation on lipid metabolism. This review provides a summary of known endogenous, naturally occurring, and synthetic ligands. The review also offers considerations from a molecular modeling perspective with which to design more specific LXRβ ligands based on the interaction energies of ligands and the important amino acid residues in the LXRβ ligand binding domain.


DOI: 10.3390/molecules22010088

PubMed ID: 28067791

Funding text

The authors gratefully acknowledge support from the NSF HBCU-UP program (HRD-1505219), the NIH R15 program (1R15GM113193-01), the NIH RISE program (5R25GM060926-10), the NSF BUILD program (5RL5GM118966-03), Louisiana Biomedical Research Network-National Institutes of Health grant P20GM103424, the NIMHD grant 2G12MD007595, and Louisiana Cancer Research Consortium (LCRC).