Michael Laura F, Schkeryantz Jeffrey M, Burris Thomas P
Lilly Research Laboratories, Lilly Corporate Center, Indianapolis, IN 46285, USA.
Mini Rev Med Chem. 2005 Aug;5(8):729-40. doi: 10.2174/1389557054553767.
Liver X receptors (LXRs) are members of the nuclear hormone receptor superfamily of ligand-activated transcription factors. Two LXRs (LXRalpha and LXRbeta) were initially characterized as orphan members of this superfamily with disparate patterns of tissue expression. These two receptors later were recognized as sterol-responsive with the ability to directly bind several oxysterol metabolites. Many LXR target genes have been identified that implicate these receptors in a variety of physiological processes including cholesterol transport and metabolism, glucose metabolism, and inflammation. Synthetic LXR ligands have been designed with the potential to treat disorders such as atherosclerosis and diabetes. In this review, we describe the potential utility of LXR ligands in the treatment of disease.
肝脏X受体(LXRs)是配体激活转录因子核激素受体超家族的成员。最初,两种LXRs(LXRα和LXRβ)被鉴定为该超家族的孤儿成员,具有不同的组织表达模式。这两种受体后来被认为是固醇反应性的,能够直接结合几种氧化固醇代谢产物。已经鉴定出许多LXR靶基因,这些基因表明这些受体参与多种生理过程,包括胆固醇转运和代谢、葡萄糖代谢以及炎症。已经设计出具有治疗动脉粥样硬化和糖尿病等疾病潜力的合成LXR配体。在这篇综述中,我们描述了LXR配体在疾病治疗中的潜在用途。