Application and interpretation of current autophagy inhibitors and activators

• Published in: Acta pharmacologica Sinica Vol. 34; no. 5; pp. 625 - 635
• Main Authors: Yang, Ya-ping, Hu, Li-fang, Zheng, Hui-fen, Mao, Cheng-jie, Hu, Wei-dong, Xiong, Kang-ping, Wang, Fen, Liu, Chun-feng
• Format: Journal Article
• Language: English
• Published: London Nature Publishing Group UK 01.05.2013; Nature Publishing Group
• Subjects: Animals; Autophagy - drug effects; Biomedical and Life Sciences; Biomedicine; Drug Discovery - methods; Humans; Immunology; Internal Medicine; Medical Microbiology; Neoplasms - drug therapy; Neoplasms - metabolism; Neurodegenerative Diseases - drug therapy; Neurodegenerative Diseases - metabolism; Pharmacology/Toxicology; Review; Vaccine; 人类疾病; 应用; 抑制剂; 激活剂; 程序性细胞死亡; 细胞程序性死亡; 自噬; 质量控制机制; cycloheximide; neurodegenerative diseases; LiCl; autophagy; Rack1 protein; ER stress inducer; lysosomal lumen alkalizer; PI3K inhibitor; cancer; rapamycin
• ISSN: 1671-4083; 1745-7254
• DOI: 10.1038/aps.2013.5

is the major intracellular degradation system, by which cytoplasmic materials are delivered to and degraded in the lyso- some. As a quality control mechanism for cytoplasmic proteins and organelles, autophagy plays important roles in a variety of human diseases, including neurodegenerative diseases, cancer, cardiovascular disease, diabetes and infectious and inflammatory diseases. The discovery of ATG genes and the dissection of the signaling pathways involved in regulating autophagy have greatly enriched our knowledge on the occurrence and development of this lysosomal degradation pathway. In addition to its role in degradation, autophagy may also promote a type of programmed cell death that is different from apoptosis, termed type II programmed cell death. Owing to the dual roles of autophagy in cell death and the specificity of diseases, the exact mechanisms of autophagy in various diseases require more investigation. The application of autophagy inhibitors and activators will help us understand the regulation of autophagy in human diseases, and provide insight into the use of autophagy-targeted drugs. In this review, we summarize the latest research on autophagy inhibitors and activators and discuss the possibility of their application in human disease therapy.