Research advance on P-glycoprotein inhibitors and the structure-activity relationship

Abstract

Abstract: P-glycoprotein (P-gp) is an important ATP-dependent transmembrane transporter, which can pump out a large number of structural and functional diverse compounds. P-gp plays a prominent role in physiological and pathological functions. It is not only crucial to drug disposition, but also one of the main causes of multidrug resistance (MDR). Therefore, developing P-gp inhibitors is significant to researches on modulation of drug pharmacokinetics and reversion of multidrug resistance. In this paper, we summarize studies on structure-activity relationship of P-gp inhibitors, which will give us important information for screening and synthesizing desirable P-gp inhibitors in the future.

Key words: P-glycoprotein, Multidrug resistance, Structure-activity relationship

CLC Number:

R969

WEN Xiao-zhou, ZHOU Fang, WU Xiao-lan, WANG Guang-ji. Research advance on P-glycoprotein inhibitors and the structure-activity relationship[J]. Chinese Journal of Clinical Pharmacology and Therapeutics, 2010, 15(7): 814-820.

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