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Tumor cells may display a multidrug resistant phenotype by overexpression of ATP-binding cassette transporters such as multidrug resistance (MDRI) p-glycoprotein, multidrug resistance protein 1 (MRP1), and breast cancer resistance protein (BCRP). Tumor cells can be intrinsically resistant to drugs or they can acquire resistance to structurally and functionally unrelated drugs on drug exposure. This phenomenon is known as multidrug resistance (MDR). In human tumor cells, several transporter proteins can be involved in MDR. These proteins, MDR1 P-gp (ABCB1), MRP1 (ABCC1), MRP2 (ABCC2), MRP3 (ABCC3), and BCRP (ABCG2), belong to the ABC transporter family. They act as efflux pumps, which result in decreased intracellular concentrations of cytotoxic drugs. BCRP is a recently discovered half-transporter that probably acts as a homo- or heterodimer in transporting cytotoxic agents. The transporter molecule is capable of transporting several anticancer drugs but has thus far been found mainly in MX-resistant cell lines.