Development of small-molecule PCSK9 inhibitors for the treatment of hypercholesterolemia

Shakir Ahamad,Shintu Mathew,Waqas A. Khan,Kishor Mohanan

Drug Discovery Today（2022）

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摘要

•PCSK9 is a novel therapeutic target for preventing and treating atherosclerosis.•Two monoclonal antibodies to inhibit PCSK9 are already in the market.•Many small molecules targeting PCSK9 have been identified in the last decade.•Currently, no small molecule drug specific to PCSK9 is in the clinical trial.•Design and therapeutic effects of small molecule PCSK9 modulators are summarized.

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关键词

Atherosclerosis,Low-density lipoprotein-cholesterol,PCSK9 inhibitors,Small-molecule drugs,Protein–protein interaction inhibitors

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