Liver X receptors in lipid metabolism: opportunities for drug discovery.
The liver X receptors (LXRs) are pivotal regulators of lipid homeostasis in mammals. These transcription factors control the expression of a battery of genes involved in the uptake, transport, efflux and excretion of cholesterol in a tissue-dependent manner. The identification of the LXRs, and an increased understanding of the mechanisms by which LXR signalling regulates lipid homeostasis in different tissues (including the liver, intestine and brain), has highlighted new opportunities for therapeutic intervention in human metabolism. New strategies for the pharmacological manipulation of LXRs and their target genes offer promise for the treatment of human diseases in which lipids have a central role, including atherosclerosis and Alzheimer's disease.
Howard Hughes Medical Institute, Department of Pathology and Laboratory Medicine, MacDonald Research Laboratories 6-770, 675 Charles E Young Drive South, Los Angeles, California 90095, USA.
Cynthia
C
Hong
Howard Hughes Medical Institute, Department of Pathology and Laboratory Medicine, MacDonald Research Laboratories 6-770, 675 Charles E Young Drive South, Los Angeles, California 90095, USA.
Peter
P
Tontonoz
D000544:Alzheimer Disease / Q000188:drug therapy / Q000378:metabolism / Q000517:prevention & control; D000818:Animals; D050197:Atherosclerosis / Q000188:drug therapy / Q000378:metabolism / Q000517:prevention & control; D001921:Brain / Q000187:drug effects / Q000378:metabolism; D002986:Clinical Trials as Topic; D015195:Drug Design; D055808:Drug Discovery; D004353:Drug Evaluation, Preclinical; D015507:Drugs, Investigational / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D006801:Humans; D000960:Hypolipidemic Agents / Q000009:adverse effects / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D007413:Intestinal Mucosa / Q000378:metabolism; D007422:Intestines / Q000187:drug effects; D050356:Lipid Metabolism / Q000187:drug effects*; D008099:Liver / Q000187:drug effects / Q000378:metabolism; D000071518:Liver X Receptors; D058990:Molecular Targeted Therapy / Q000009:adverse effects; D009419:Nerve Tissue Proteins / Q000037:antagonists & inhibitors / Q000378:metabolism; D009474:Neurons / Q000187:drug effects / Q000378:metabolism; D018697:Nootropic Agents / Q000009:adverse effects / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D057093:Orphan Nuclear Receptors / Q000037:antagonists & inhibitors* / Q000378:metabolism; D020033:Protein Isoforms / Q000037:antagonists & inhibitors / Q000378:metabolism; D015398:Signal Transduction / Q000187:drug effects
D015507:Drugs, Investigational; D000960:Hypolipidemic Agents; D000071518:Liver X Receptors; D009419:Nerve Tissue Proteins; D018697:Nootropic Agents; D057093:Orphan Nuclear Receptors; D020033:Protein Isoforms