Exelixis, Inc., San Diego, CA, USA.
J Lipid Res. 2010 May;51(5):900-6. doi: 10.1194/jlr.M900096.
The liver X receptors LXRalpha and LXRbeta play critical roles in maintaining lipid homeostasis by functioning as transcription factors that regulate genetic networks controlling the transport, catabolism, and excretion of cholesterol. The studies described in this report examine the individual anti-atherogenic activity of LXRalpha and LXRbeta and determine the ability of each subtype to mediate the biological response to LXR agonists. Utilizing individual knockouts of LXRalpha and LXRbeta in the Ldlr(-/-) background, we demonstrate that LXRalpha has a dominant role in limiting atherosclerosis in vivo. Functional studies in macrophages indicate that LXRalpha is required for a robust response to LXR ligands, whereas LXRbeta functions more strongly as a repressor. Furthermore, selective knockout of LXRalpha in hematopoietic cells and rescue experiments indicate that the anti-atherogenic activity of this LXR subtype is not restricted to macrophages. These studies indicate that LXRalpha plays a selective role in limiting atherosclerosis in response to hyperlipidemia.
肝 X 受体 LXRα 和 LXRβ 通过作为转录因子发挥作用,调节控制胆固醇转运、分解代谢和排泄的基因网络,从而在维持脂质稳态方面发挥关键作用。本报告中描述的研究检查了 LXRα 和 LXRβ 的个体抗动脉粥样硬化活性,并确定了每种亚型介导 LXR 激动剂的生物学反应的能力。利用 Ldlr(-/-)背景下的 LXRα 和 LXRβ 个体敲除,我们证明 LXRα 在体内限制动脉粥样硬化中起主导作用。巨噬细胞中的功能研究表明,LXRα 是对 LXR 配体产生强烈反应所必需的,而 LXRβ 作为抑制剂的作用更强。此外,选择性敲除造血细胞中的 LXRα 和挽救实验表明,这种 LXR 亚型的抗动脉粥样硬化活性不仅限于巨噬细胞。这些研究表明,LXRα 在响应高血脂症限制动脉粥样硬化方面发挥选择性作用。