Kang Sung-Min, Kim Do-Hee
College of Pharmacy, Duksung Women's University, Seoul 01369, Korea.
College of Pharmacy, Jeju National University, Jeju 63243, Korea.
Life (Basel). 2021 Jun 4;11(6):526. doi: 10.3390/life11060526.
Autophagy is a lysosome-dependent intracellular degradation machinery that plays an essential role in the regulation of cellular homeostasis. As many studies have revealed that autophagy is related to cancer, neurodegenerative diseases, metabolic diseases, and so on, and it is considered as a promising drug target. Recent advances in structural determination and computational technologies provide important structural information on essential autophagy-related proteins. Combined with high-throughput screening methods, structure-activity relationship studies have led to the discovery of molecules that modulate autophagy. In this review, we summarize the recent structural studies on autophagy-related proteins and the discovery of modulators, indicating that targeting autophagy can be utilized as an effective strategy for novel drug development.
自噬是一种依赖溶酶体的细胞内降解机制，在细胞稳态调节中起着至关重要的作用。许多研究表明，自噬与癌症、神经退行性疾病、代谢性疾病等相关，并且它被认为是一个有前景的药物靶点。结构测定和计算技术的最新进展提供了关于自噬相关关键蛋白的重要结构信息。结合高通量筛选方法，构效关系研究已导致发现了调节自噬的分子。在本综述中，我们总结了自噬相关蛋白的近期结构研究以及调节剂的发现，表明靶向自噬可作为新型药物开发的有效策略。
