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Discovery of a small-molecule activator of beclin-1 that induces autophagy-associated cell death and apoptosis in triple negative breast cancer
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Rong-yan ZHAO1, Wen-ke JIN1, 2, Xing JIANG1, Zhao-xin YUAN1, 2, Bo LIU2, *, Lei-lei FU1, *
Acta Pharmaceutica Sinica | 2021, 56(5) : 1369 - 1383
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Acta Pharmaceutica Sinica | 2021, 56(5): 1369-1383
• Original Articles •
Discovery of a small-molecule activator of beclin-1 that induces autophagy-associated cell death and apoptosis in triple negative breast cancer
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Rong-yan ZHAO1, Wen-ke JIN1, 2, Xing JIANG1, Zhao-xin YUAN1, 2, Bo LIU2, *, Lei-lei FU1, *
Affiliations
  • 1. School of Life Science and Engineering, Southwest Jiaotong University, Chengdu 610031, China
  • 2. State Key Laboratory of Biotherapy and Cancer Center, Sichuan University, Chengdu 610041, China
Published: 2021-05-12 doi: 10.16438/j.0513-4870.2021-0265
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Autophagy is a lysosomal degradation pathway, and plays a crucial role in cellular homeostasis, development, immunity, tumor suppression, metabolism, prevention of neurodegeneration, and lifespan extension. Thus, pharmacological stimulation of autophagy may be an effective approach for preventing or treating certain human diseases and/or aging. Here, combined with allosteric site identification methods, high-throughput virtual screening, and in vitro activity evaluation, we found that compound 10 can activate autophagy and has good anti-MDA-MB-231 cell proliferation activity (the half maximal inhibitory concentration IC50=8.25±1.53 μmol·L-1). Subsequently, molecular docking, molecular dynamics simulation, and immunoblotting assay demonstrate that compound 10 can target and activate beclin-1. In vitro studies have shown that compound 10 can induce autophagy-associated cell death in MDA-MB-231 cells. In addition, it was found that compound 10 can induce apoptosis in MDA-MB-231 cells. Taken together, we identified the candidate compound 10 as an effective and selective targeting beclin-1 to activate autophagy as a lead compound, which provide a reference for further development and optimization of small molecule drugs targeting beclin-1 to activate autophagy for clinical treatment.

triple negative breast cancer  /  beclin-1  /  small-molecule activator  /  autophagy  /  apoptosis
Rong-yan ZHAO, Wen-ke JIN, Xing JIANG, Zhao-xin YUAN, Bo LIU, Lei-lei FU. Discovery of a small-molecule activator of beclin-1 that induces autophagy-associated cell death and apoptosis in triple negative breast cancer[J]. Acta Pharmaceutica Sinica, 2021 , 56 (5) : 1369 -1383 . DOI: 10.16438/j.0513-4870.2021-0265
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Article Info
doi: 10.16438/j.0513-4870.2021-0265
  • Receive Date：2021-02-23
  • Online Date：2025-12-18
  • Published：2021-05-12
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  • Received：2021-02-23
  • Revised：2021-03-22
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Affiliations
    1. School of Life Science and Engineering, Southwest Jiaotong University, Chengdu 610031, China
    2. State Key Laboratory of Biotherapy and Cancer Center, Sichuan University, Chengdu 610041, China
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小菇科 Mycenaceae 2 12 5.74 丝盖伞属 Inocybe 5 2.39
多孔菌科 Polyporaceae 8 14 6.70 蜡蘑属 Laccaria 5 2.39
红菇科 Russulaceae 3 23 11.00 小皮伞属 Marasmius 6 2.87
小菇属 Mycena 11 5.26
光柄菇属 Pluteus 5 2.39
红菇属 Russula 17 8.13
栓菌属 Trametes 5 2.39
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