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Components of the extracellular environment can be transported into cells by molecular mechanisms collectively termed endocytosis. Cells typically use a multitude of such internalization pathways. These endocytic transport pathways have a wide range of implications for physiological regulation as well as pathological processes. Many infectious diseases, for example, involve internalization of the pathogen into the cell as part of the infection process. Selective interference with the endocytic transport of a microbe, thus, represents a therapeutic strategy that may prevent infections or decrease the rate of their progression. Herein, we provide a brief review of strategies for discovery of novel anti-infection drugs and their pharmacological implications.