P-glycoprotein and membrane roles in multidrug resistance.

P-glycoprotein and membrane roles in multidrug resistance.

Future Med Chem. 2015 Jun;7(7):929-946

Authors: Ferreira RJ, Dos Santos DJ, Ferreira MJ

Abstract
Multidrug-resistance (MDR) phenomena are a worldwide health concern. ATP-binding cassette efflux pumps as P-glycoprotein have been thoroughly studied in a frantic run to develop new efflux modulators capable to reverse MDR phenotypes. The study of efflux pumps has provided some key aspects on drug extrusion, however the answers could not be found solely on ATP-binding cassette transporters. Its counterpart - the plasma membrane - is now emerging as a critical structure able to modify drug behavior and efflux pump activity. Alterations in the membrane surrounding P-glycoprotein are now known to modulate drug efflux, with membrane-related biophysical, biochemical and mechanical aspects further increasing the complexity of an already multifaceted phenomena. This review summarizes the main knowledge comprising the plasma membrane role in MDR.

PMID: 26061109 [PubMed - as supplied by publisher]