Liver X receptors and atherosclerosis.
Cardiovascular disease, the primary cause of death and illness in the industrialized world, is typically due to complications of atherosclerosis, a multifactorial disease of the arterial intima. The liver X receptors (LXRs), LXRalpha and LXRbeta, are intracellular receptors that appear to play an important role in protection against atherosclerosis; however, LXR activation also leads to a dramatic increase in liver and serum triglycerides. This presents a challenge to developing drugs via these targets. This article discusses the role of LXRs in atherosclerosis and lipid regulation and the possibility of designing LXR ligands that may be anti-atherogenic without side effects.
Lala
Deepak S
DS
Pfizer Global Research and Development, Building 26 Room 261N, 2800 Plymouth Road, Ann Arbor, MI 48105, USA. deepak.s.lala@pfizer.com
D000818:Animals; D001161:Arteriosclerosis / Q000188:drug therapy / Q000235:genetics / Q000473:pathology / Q000503:physiopathology*; D002784:Cholesterol / Q000378:metabolism; D004268:DNA-Binding Proteins; D006801:Humans; D050356:Lipid Metabolism; D000071518:Liver X Receptors; D057093:Orphan Nuclear Receptors; D018160:Receptors, Cytoplasmic and Nuclear / Q000187:drug effects / Q000235:genetics / Q000502:physiology*; D014280:Triglycerides / Q000378:metabolism
D004268:DNA-Binding Proteins; D000071518:Liver X Receptors; C000605213:NR1H3 protein, human; D057093:Orphan Nuclear Receptors; D018160:Receptors, Cytoplasmic and Nuclear; D014280:Triglycerides; D002784:Cholesterol