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Chinese Journal of Clinical Pharmacology and Therapeutics ›› 2022, Vol. 27 ›› Issue (8): 946-954.doi: 10.12092/j.issn.1009-2501.2022.08.014

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

LI Miao1, YU Qinwei1, JIANG Zhenzhou1, ZHANG Luyong1,2   

  1. 1China Pharmaceutical University, New Drug Screening Center of Institute of Pharmaceutical Sciences, Nanjing 210009, Jiangsu, China; 2Guangdong Pharmaceutical University, New Drug Research and Development Center, Guangzhou 510006, Guangdong, China  
  • Received:2022-02-24 Revised:2022-05-17 Online:2022-08-26 Published:2022-09-13

Abstract: 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.

Key words: LDLR, regulation mechanism, LDLR related diseases, drug research progress

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