Knockdown of caveolin-1 decreases activity of breast cancer resistance protein (BCRP/ABCG2) and increases chemotherapeutic sensitivity.

The ATP-binding cassette transporter breast cancer resistance protein (BCRP/ABCG2) is supposed to be a major determinant of the multidrug resistance phenotype of tumors by extruding chemically diverse cytostatic drugs out of tumor cells. BCRP physically and possibly also functionally interacts with caveolin-1 (CAV1, encoded by Cav1), an integral membrane protein of lipid rafts important for signal transduction and membrane trafficking. Moreover, Cav1 is linked to an aggressive phenotype of cancer cells in various tumors.