First Insight into the Symmetry and Flexibility of Membrane Efflux Pump P-Glycoprotein by Novel Bifunctional Modulators

摘要

Multidrug resistance(MDR)is an increasingly common problem in the treatment of infectious diseases and cancer.Transmembrane efflux pumps play a role in the MDR of bacteria,viruses,fungi and cancer.The MDR efflux pumps mainly found in cancer cells belong to the ABC-transporter family.P-glycoprotein(P-gp)causes the highest incidence of resistance,followed by multidrug resistance-associated protein(MRP)subtypes,such as MRP1 and MRP2.P-gp was also discovered to be causative agent for viral resistance to AIDS treatment,because peptidic inhibitors of HIV protease as a therapeutic target in AIDS treatment were found to be P-gp substrates.