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Ligands of Therapeutic Utility for the Liver X Receptors

Department of Chemistry and RCMI Cancer Research Center, Xavier University of Louisiana, New Orleans, LA 70125, USA
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Academic Editor: Derek J. McPhee
Molecules 2017, 22(1), 88; https://doi.org/10.3390/molecules22010088
Received: 31 October 2016 / Revised: 29 December 2016 / Accepted: 30 December 2016 / Published: 5 January 2017
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. View Full-Text
Keywords: liver X receptors; LXRα; LXRβ specific ligands; atherosclerosis; diabetes; Alzheimer’s disease; cancer; lipid metabolism; molecular modeling; interaction energy liver X receptors; LXRα; LXRβ specific ligands; atherosclerosis; diabetes; Alzheimer’s disease; cancer; lipid metabolism; molecular modeling; interaction energy
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Komati, R.; Spadoni, D.; Zheng, S.; Sridhar, J.; Riley, K.E.; Wang, G. Ligands of Therapeutic Utility for the Liver X Receptors. Molecules 2017, 22, 88.

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