Vesicular coat proteins mediate the formation of nascent vesicles and select the cargo to be incorporated therein.

As additional coat proteins are discovered that regulate vesicular traffic along very specific intracellular pathways, the possibility looms of regulating the intracellular trafficking and targeting of therapeutic agents by modulation of the action of vesicular coat proteins.

Examples are provided of coat proteins thought to regulate the trafficking of pharmaceutically relevant molecules via clathrin-mediated endocytosis, caveolae-mediated endocytosis, and transcytosis.

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 clathrin