Year: 2017
Type: review
Abstract: 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.
Source: Molecules
Institution: Xavier University of Louisiana
Language: English
Subfield: Surgery
Field: Medicine
Domain: Health Sciences
Open Access status: gold
Estimated APC paid: $3,258
Awards: BUILD at Xavier, Project Pathways II, BUILD at Xavier, Project Pathways II, G2070940364, Generation of Liver X Receptor Agonists with LXRb Subtype Selectivity using Modern Computational and Chemical Synthetic Methods, Xavier RCMI Center for Cancer Research , Research Initiation Award: Characterization of Crystal Structures of Novel Materials using State-of the-Art Computational Techniques and Applications, G6097516853, RISE Option II at Xavier University of Louisiana, G7088262357, Project Pathways: Research Enrichment Core, Louisiana Biomedical Research Network
OpenAlex ID: W2570267130