Clermont Université, Université Blaise Pascal, Génétique Reproduction et Développement, BP 10448, F-63000 Clermont-Ferrand, France.
Mol Cell Endocrinol. 2012 Apr 4;351(2):129-41. doi: 10.1016/j.mce.2011.08.036. Epub 2011 Sep 1.
Liver X receptors (LXR) are members of the nuclear receptor family. As activated transcription factors, their putative association with human diseases makes them promising pharmacological targets because of the large potential to develop ligands. LXR are mainly considered as intracellular cholesterol "sensors" whose activation leads to decreased plasma cholesterol. They also modulate numerous physiological functions: fatty acid synthesis and metabolism, glucose homeostasis, steroidogenesis, immunity, and neurological homeostasis. LXR-deficiency in mouse results in several phenotypes mimicking pathological conditions in humans. This review will be focused on the various natural and synthetic LXR agonists and antagonists. Putative clinical targets including atherosclerosis, diabetes, Alzheimer's disease, skin disorders, and cancer will be covered.
肝 X 受体 (LXR) 是核受体家族的成员。作为激活的转录因子，它们与人类疾病的潜在关联使它们成为有前途的药物靶点，因为开发配体的潜力巨大。LXR 主要被认为是细胞内胆固醇的“传感器”，其激活导致血浆胆固醇降低。它们还调节许多生理功能：脂肪酸合成和代谢、葡萄糖稳态、类固醇生成、免疫和神经稳态。小鼠的 LXR 缺乏会导致多种表型，这些表型模拟人类的病理状况。本综述将重点介绍各种天然和合成的 LXR 激动剂和拮抗剂。涵盖的潜在临床靶点包括动脉粥样硬化、糖尿病、阿尔茨海默病、皮肤疾病和癌症。
