Ivanov Andrei I
Department of Human and Molecular Genetics, VCU Institute of Molecular Medicine, Virginia Commonwealth University, Goodwin Laboratory, 401 College Street, 980035, Richmond, VA, 23298, USA,
Methods Mol Biol. 2014;1174:3-18. doi: 10.1007/978-1-4939-0944-5_1.
Pharmacological inhibitors of vesicle trafficking possess great promise as valuable analytical tools for the study of a variety of biological processes and as potential therapeutic agents to fight microbial infections and cancer. However, many commonly used trafficking inhibitors are characterized by poor selectivity that diminishes their use in solving basic problems of cell biology or drug development. Recent high-throughput chemical screens intensified the search for novel modulators of vesicle trafficking, and successfully identified a number of small molecules that inhibit exocytosis and endocytosis in different types of mammalian cells. This chapter provides a systematic overview of recently discovered inhibitors of vesicle trafficking. It describes cellular effects and mechanisms of action of novel inhibitors of exocytosis and endocytosis. Furthermore, it pays special attention to the selectivity and possible off-target effects of these inhibitors.
囊泡运输的药理学抑制剂作为研究各种生物过程的有价值分析工具以及对抗微生物感染和癌症的潜在治疗剂具有巨大潜力。然而，许多常用的运输抑制剂具有选择性差的特点，这限制了它们在解决细胞生物学基本问题或药物开发中的应用。最近的高通量化学筛选加强了对囊泡运输新型调节剂的搜索，并成功鉴定出了一些能抑制不同类型哺乳动物细胞胞吐作用和内吞作用的小分子。本章系统概述了最近发现的囊泡运输抑制剂。它描述了胞吐作用和内吞作用新型抑制剂的细胞效应和作用机制。此外，它特别关注这些抑制剂的选择性和可能的脱靶效应。
