数字农科院2.0

The SAR and action mechanisms of autophagy inhibitors that eliminate drug resistance

文献类型： 外文期刊

作者： Ye W.;Fan C.;Fu K.;Wang X.;Lin J.;Nian S.;Liu C.;Zhou W.

作者机构：

关键词： Action mechanisms;Autophagy;Autophagy inhibitors;Drug resistance;Structure-activity relationships (SARs)

期刊名称： European Journal of Medicinal Chemistry

ISSN： 0223-5234

年卷期： 2022 年 244 卷

页码：

收录情况： SCIE（2022版）

摘要： Autophagy is an essential homeostatic and catabolic process crucial for the degradation or recycling of proteins and cellular components. Drug resistance has been demonstrated to be closely implicated in increased autophagy. Autophagy inhibition to reverse drug resistance involves in the five stages of autophagy, including phagophore initiation, vesicle nucleation, vesicle elongation, vesicle fusion and cargo degradation. Herein, emphases were placed on discussions on the targets responsible for the upstream phagophore initiation and nucleation of autophagosome, as well as the ones mediating the downstream autophagosome and lysosome fusion and cargo degradation. The structure-activity relationships (SARs) and action mechanisms of the corresponding target-based small molecule autophagy inhibitors were analyzed and delineated. This review will provide a promising guidance for the design and optimization of drug-like scaffolds in the discovery of autophagy inhibitors able to eliminate drug resistance. © 2022 Elsevier Masson SAS

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