There has been an exponential growth in caveolae research since the early 1990s. The caveolae membrane system comprises unique lipid and protein domains, and fulfills a role in a wide range of processes. At the plasma membrane caveolae serve to compartmentalise and integrate a wide range of signal transduction processes. A key structural and functional protein for caveolae is caveolin. Caveolin proteins possess a ‘scaffolding’ domain which for caveolins-1 and -3 appear central to many of the reported signal regulation functions for caveolae. Caveolae or caveolin protein are increasingly implicated in the molecular pathology of a number of diseases. Opportunities exist for basic and applied investigators working within the pharmaceutical sciences to exploit the caveolae membrane system to identify novel pharmacological targets and therapeutic strategies, including the delivery of pharmacologically active caveolin based peptides.