中文摘要：

P糖蛋白（P-glycoprotein,P-gp）是一种多药外排转运体,对控制各种抗癌药物的生物学活性具有重要意义。P-gp转运体作为生理屏障阻滞药物渗透,从而使药物发挥效应受限。传统的化疗增敏剂通过对转运体的调节可有效改善抗肿瘤药物的药代动力学并逆转多药耐药。本文将简要概述近年来有关P-gp与配体相互作用的结构信息以及肿瘤耐药逆转策略的研究进展。

英文摘要：

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.