Fiévet C, Staels B
Institut Pasteur de Lille, Lille, F-59019, France.
Biochem Pharmacol. 2009 Apr 15;77(8):1316-27. doi: 10.1016/j.bcp.2008.11.026. Epub 2008 Dec 3.
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.
肝脏X受体(LXRs)是核受体,在调节参与脂质代谢的基因表达中起关键作用。LXRs的配体激活通过多种协同作用改善胆固醇稳态,这一功能可能部分解释了在动物模型中报道的LXR激活对动脉粥样硬化的保护作用。然而,LXR激活也可能诱发不良副作用,如脂肪生成和高甘油三酯血症。本文综述了开发LXR调节剂作为动脉粥样硬化治疗药物的潜力。