Multidrug Resistance Fluorometric Assay Kit - 100 assays

The phenomenon of resistance of tumors to chemically unrelated anticancer drugs, termed multidrug resistance, represents the most formidable challenge to the field of oncology. Multidrug resistance can be present at the time of diagnosis, or can be acquired after initial treatment and remission of a cancer. Although multiple mechanisms mediate multidrug resistance, the first mediator of multidrug resistance to be characterized at the molecular level was MDR1, also known as P-glycoprotein (Pgp) and ABCB1 (Gottesman et al., 2002). MDR1 mediates resistance to various classes of chemotherapeutic agents, including vinca alkaloids (vinblastine and vincristine), anthracyclines, paclitaxel and etoposide, by actively pumping the drugs from the cytosol and plasma membrane into the extracellular space. The molecular structure of MDR1 consists of 12 transmembrane domains that form a drug-binding pore, and two cytoplasmic ATP-binding cassettes. At least nine proteins related to MDR1 have been characterized to date and shown to mediate efflux of small molecules from cells (Gottesman et al., 2002). Two of these MDR1 relatives, multidrug-resistance-associated protein 1 (MRP1, or ABCC1) and breast cancer resistance protein (BCRP, or ABCG2), have also been demonstrated to mediate multidrug resistance in tumor cells. These proteins belong to a larger family of ABC (ATP-binding cassette) proteins that function as transporters of ions, nutrients, and peptides. Application:The Multidrug Resistance Direct Dye Efflux Activity Kit is designed to directly measure the functional activity of MDR1, MRP1 and BCRP by assaying for the ability of the cell to extrude fluorescent transport substrates of these proteins. The kit can be used to measure relative amounts of MDR1, MRP and BCRP activity between different cell populations. In addition, dye efflux assays can be used to assess the ability of unlabeled small molecules to serve as transport substrates for MDR1, MRP1 and BCRP and the ability of candidate inhibitors to block the function of these proteins. Method: Species: Storage:2-8°C