LDLR的调控机制及其相关疾病与药物研究进展  

Regulatory mechanism of LDLR and research progress of its related diseases and drugs

作　　者：李苗 俞沁玮 江振洲 张陆勇 LI Miao;YU Qinwei;JIANG Zhenzhou;ZHANG Luyong(China Pharmaceutical University,New Drug Screening Center of Institute of Pharmaceutical Sciences,Nanjing 210009,Jiangsu,China;Guangdong Pharmaceutical University,New Drug Research and Development Center,Guangzhou 510006,Guangdong,China)

机构地区：[1]中国药科大学,药物科学研究院新药筛选中心,江苏南京210009 [2]广东药科大学,新药研发中心,广东广州510006

出　　处：《中国临床药理学与治疗学》2022年第8期946-954,共9页Chinese Journal of Clinical Pharmacology and Therapeutics

摘　　要：胆固醇是机体内一种重要的脂质成分,它不仅参与形成细胞膜而且是合成胆汁酸及类固醇激素的原料。低密度脂蛋白受体(low density lipoprotein receptor,LDLR)参与胆固醇的代谢过程,在维持机体细胞胆固醇稳态中发挥着重要作用。LDLR的表达受到转录、转录后及翻译后水平的精确调节,其表达失调将导致多种疾病的发生发展。本文主要从LDLR的分子调节机制、LDLR表达失调导致的靶器官损害及以LDLR为靶点的药物研发进展等方面加以综述,为进一步深入了解脂代谢紊乱相关疾病的进展提供理论依据,也为开发更有效、副作用更少的LDLR靶点药物提供新的见解。Cholesterol is an important lipid component in the body,which not only participates in the formation of cell membranes,but also is the raw material for the synthesis of bile acids and steroid hormones.Low density lipoprotein receptor(LDLR)is involved in cholesterol metabolism and plays an important role in maintaining the cholesterol homeostasis of organism cells.The expression of LDLR is precisely regulated by transcription,post-transcription and post-translation,and the imbalance of ldlr expression will lead to the occurrence and development of many diseases.In this paper,the molecular regulation mechanism of LDLR,the damage of target organs caused by the imbalance of LDLR expression and the research and development progress of drugs targeting LDLR are reviewed,which provides theoretical basis for further understanding of the progress of diseases related to lipid metabolism disorder and new insights for developing drugs targeting LDLR with more effective and less side effects.

关 键 词：低密度脂蛋白受体 调控机制 LDLR相关疾病 药物研究进展 

分 类 号：R329.2[医药卫生—人体解剖和组织胚胎学] R966[医药卫生—基础医学]