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Liver X receptor modulators: Effects on lipid metabolism and potential use in the treatment of atherosclerosis |
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| Authors: | C. Fié vet,B. Staels |
| Affiliation: | a Institut Pasteur de Lille, Lille, F-59019, France b Inserm, U545, Lille, F-59019, France c Université de Lille 2, Faculté des Sciences Pharmaceutiques et Biologiques et Faculté de Médecine, Lille, F-59006, France |
| Abstract: | Liver X receptors (LXRs) are nuclear receptors that play a crucial role in regulating the expression of genes involved in lipid metabolism. Ligand activation of LXRs improves cholesterol homeostasis via multiple coordinated effects, and this function is likely to explain in part the protective effects of LXR activation on atherosclerosis reported in animal models. However, LXR activation may also induce undesirable side effects, such as lipogenesis and hypertriglyceridemia. This review discusses the potential to develop LXR modulators as therapeutic agents for atherosclerosis. |
| Keywords: | LXR, Liver X receptor ABC, ATP-binding cassette transporter NPC1L1, Niemann-Pick C1 like 1 LDLR, LDL receptor SREBP, sterol regulatory element-binding protein SQS, squalene synthase RCT, reverse cholesterol transport HDL, high-density lipoproteins Apo, apolipoprotein PLTP, phospholipids transfer protein CETP, cholesteryl ester transfer protein LPL, lipoprotein lipase SCD1, stearoyl-coenzyme A desaturase FAS, fatty acid synthase ACC, acetyl-coA carboxylase ChREBP, carbohydrate response element binding protein Angptl3, angiopoietin-like protein 3 SLXRM, selective LXR modulator RC, riccardin AIM, apoptosis inhibitory factor |
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