Detection of the MDR1 P-Glycoprotein Expression and Function

Acquired and intrinsic multidrug resistance is the major reason for the failure of anticancer chemotherapy. The most important component of clinical multidrug resistance is mediated by P-glycoprotein (Pgp), an ABC transporter encoded by the MDR1 gene and expressed on the membrane of tumor and normal cells. Sensitive and reproducible detection of Pgp expression and function are critical for the development of new MDR1 drugs and clinical protocols aimed at modulating Pgp-mediated multidrug resistance. The most commonly used methods for detecting Pgp distribution and functional activity have major flaws when used in routine clinical diagnostics. In this chapter, we describe and compare these techniques and introduce a new method for simultaneous detection of Pgp expression and function—the UIC2 Shift assay.