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Liver X receptors and atherosclerosis
1Pfizer Global Research and Development, Building 26 Room 261N, 2800 Plymouth Road, Ann Arbor, MI 48105, USA. deepak.s.lala@pfizer.com
Abstract:
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.