Dave Vivek Priy, Kaul Deepak
Vivek Priy Dave, Deepak Kaul, Department of Experimental Medicine and Biotechnology, Post Graduate Institute of Medical Education and Research, Chandigarh 160012, India.
World J Cardiol. 2010 Jun 26;2(6):140-9. doi: 10.4330/wjc.v2.i6.140.
Crosstalk between lipid peroxidation and inflammation is known to be a pathognomonic feature for the development of coronary heart disease (CHD). In this regard ligand activated liver X receptor (LXR)-α has emerged as a key molecular switch by its inherent ability to modulate an array of genes involved in these two fundamental cellular processes. In addition, LXR-α has also been found to play a role in hepatic lipogenesis and innate immunity. Although several lines of evidence in experimental model systems have established the atheroprotective nature of LXR-α, human subjects have been reported to possess a paradoxical situation in which increased blood cellular LXR-α gene expression is always accompanied by increased coronary occlusion. This apparent paradox was resolved recently by the finding that CHD patients possess a deregulated LXR-α transcriptome due to impaired ligand-receptor interaction. This blood cellular mutated LXR-α gene expression correlated specifically with the extent of coronary occlusion and hence need is felt to devise new synthetic ligands that could restore the function of this mutated LXR-α protein in order to modulate genes involved in reverse cholesterol transport and suppression of the inflammatory response leading to the effective treatment of CHD.
脂质过氧化与炎症之间的相互作用是冠心病(CHD)发展的一个特征性表现。在这方面,配体激活的肝脏X受体(LXR)-α已成为一个关键的分子开关,因为它具有调节参与这两个基本细胞过程的一系列基因的内在能力。此外,还发现LXR-α在肝脏脂肪生成和固有免疫中发挥作用。尽管实验模型系统中的多项证据证实了LXR-α的抗动脉粥样硬化特性,但据报道,人类受试者存在一种矛盾的情况,即血细胞中LXR-α基因表达增加总是伴随着冠状动脉阻塞增加。最近发现冠心病患者由于配体-受体相互作用受损而导致LXR-α转录组失调,从而解决了这一明显的矛盾。这种血细胞中突变的LXR-α基因表达与冠状动脉阻塞程度密切相关,因此需要设计新的合成配体,以恢复这种突变的LXR-α蛋白的功能,从而调节参与逆向胆固醇转运和抑制炎症反应的基因,有效治疗冠心病。