Multi-drug resistance efflux protein P-glycoprotein

P-glycoprotein (P-gp), a 180 kDa membrane protein, is known to be involved in multi-drug resistance, a major obstacle in tumor chemotherapy. Evidence has been presented that this protein, which functions as an efflux pump, interacts with its substrates within the plasma membrane. The localization of P-gp in cultured cells under various conditions (e.g. cholesterol depletion) and the efflux of fluorescent P-gp substrates out of cells are studied by confocal laser scanning microscopy. With easily accessible raft preparations of P-gp-overexpressing cells, we developed an assay system to study the influence of compounds on the ATPase activity of P-gp. To investigate the relationship between drug/lipid bilayer, drug/P-gp and lipid/P-gp interactions, respectively, P-gp is reconstituted in virtually detergent-free proteoliposomes of defined lipid compositions which can be tested in the previously developed ATPase assay.

ETH Research Database: id 8913

Contacts: Prof. Dr. Heidi Wunderli-Allenspach, Dr. Stefanie Krämer