首页|Research on Hepatocyte Regulation of PCSK9-LDLR and Its Related Drug Targets

Research on Hepatocyte Regulation of PCSK9-LDLR and Its Related Drug Targets

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The prevalence of hyperlipidemia has increased significantly due to genetic,dietary,nutritional and pharmacological factors,and has become one of the most common pathological conditions in humans.Hyperlipidemia can lead to a range of diseases such as atherosclerosis,stroke,coronary heart disease,myocardial infarction,diabetes,and kidney failure,etc.High circulating low-density lipoprotein cholesterol(LDL-C)is one of the causes of hyperlipidemia.LDL-C in the blood binds to LDL receptor(LDLR)and regulates cholesterol homeostasis through endocytosis.In contrast,proprotein convertase subtilisin/kexin type 9(PCSK9)mediates LDLR degradation via the intracellular and extracellular pathways,leading to hyperlipidemia.Targeting PCSK9-synthesizing transcription factors and downstream molecules are important for development of new lipid-lowering drugs.Clinical trials regarding PCSK9 inhibitors have demonstrated a reduction in atherosclerotic cardiovascular disease events.The purpose of this review was to explore the target and mechanism of intracellular and extracellular pathways in degradation of LDLR and related drugs by PCSK9 in order to open up a new pathway for the development of new lipid-lowering drugs.

hyperlipidemiaproprotein convertase subtilisin/kexin type 9low-density lipoprotein receptorintracellular pathwayextracellular pathway

LIU Su-su、YU Tong、QIAO Yan-fang、GU Shu-xiao、CHAI Xin-lou

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School of Traditional Chinese Medicine,Beijing University of Chinese Medicine,Beijing(102401),China

National Science and Technology Major Special Project Based on Big Data Research and Development of New Chinese Medicine Drugs

2019ZX09201004-001-021

2024

10.1007/s11655-023-3545-z

中国结合医学杂志(英文版)
中国中西医结合学会 中国中医研究院

中国结合医学杂志(英文版)

CSTPCD
影响因子：1.056
ISSN：1672-0415
年,卷(期)：2024.30(7)