Structure basis of P-gp-ligands interaction and reversal of P-gp-mediated multidrug resistance / 国际药学研究杂志

ABSTRACT

P-glycoprotein(P-gp) is a multi-drug efflux transporter that plays a significant role in governing the bioavailability of various anti-cancer drugs. P-gp transporter impedes the permeability of drugs through physiological barriers resulting in limited pharmacological response. Modulation of this efflux transporter by various traditional "chemosensitizers" forms a distinctive approach in improving pharmacokinetics and conquering drug resistance. This review summarizes the recent advances in structural information of P-gp interactions with investigated ligands and new strategies to improve the poor efficiency in chemotherapy.