Ivanov Andrei I
Department of Medicine, Gastroenterology and Hepatology Division, University of Rochester School of Medicine and Dentistry, Rochester, NY, USA.
Methods Mol Biol. 2008;440:15-33. doi: 10.1007/978-1-59745-178-9_2.
Eukaryotic cells constantly form and internalize plasma membrane vesicles in a process known as endocytosis. Endocytosis serves a variety of housekeeping and specialized cellular functions, and it can be mediated by distinct molecular pathways. Among them, internalization via clathrin-coated pits, lipid raft/caveolae-mediated endocytosis and macropinocytosis/phagocytosis are the most extensively characterized. The major endocytic pathways are usually distinguished on the basis of their differential sensitivity to pharmacological/chemical inhibitors, although the possibility of nonspecific effects of such inhibitors is frequently overlooked. This review provides a critical evaluation of the selectivity of the most widely used pharmacological inhibitors of clathrin-mediated, lipid raft/caveolae-mediated endocytosis and macropinocytosis/phagocytosis. The mechanisms of actions of these agents are described with special emphasis on their reported side effects on the alternative internalization modes and the actin cytoskeleton. The most and the least-selective inhibitors of each major endocytic pathway are highlighted.
真核细胞通过一种称为内吞作用的过程不断形成并内化质膜囊泡。内吞作用具有多种维持细胞正常功能和特殊的细胞功能，并且可以由不同的分子途径介导。其中，通过网格蛋白包被小窝的内化作用、脂筏/小窝介导的内吞作用以及巨胞饮作用/吞噬作用是特征最为明确的。主要的内吞途径通常根据它们对药理/化学抑制剂的不同敏感性来区分，尽管此类抑制剂非特异性效应的可能性常常被忽视。本综述对网格蛋白介导的、脂筏/小窝介导的内吞作用以及巨胞饮作用/吞噬作用中最广泛使用的药理抑制剂的选择性进行了批判性评估。描述了这些药物的作用机制，特别强调了它们对替代内化模式和肌动蛋白细胞骨架的报道副作用。突出了每种主要内吞途径中选择性最高和最低的抑制剂。
