Advances in P-glycoprotein inhibitor research
- VernacularTitle:P-糖蛋白抑制剂研究进展
- Author:
Yi-Xin ZENG
1
;
Jian-Dong JIANG
;
Wei-Jia KONG
Author Information
- Keywords: P-glycoprotein; ATP-binding cassette transporter; multidrug resistance; drug interactions; natural products; excip-ients
- From: Chinese Pharmacological Bulletin 2024;40(12):2201-2206
- CountryChina
- Language:Chinese
- Abstract: Overexpression of P-glycoprotein(P-gp)is one of the major causes of therapeutic resistance to a variety of drugs,in-cluding antitumor drugs.P-gp has a wide range of substrates that are capable of expelling drugs from the cell via a twist-squeeze mechanism,leading to drug resistance.To address the problem of P-gp-mediated multidrug resistance,several inhibitors are being investigated.This article reviews the current small mole-cule compounds,natural source compounds and pharmaceutical excipients capable of inhibiting P-gp,and summarizes the cur-rent mechanisms of action of P-gp inhibitors,which are mainly competitive or non-competitive inhibition,stimulation of ATPase activity,down-regulation of expression,and metamorphic modu-lation.Currently,it is mainly the drug interactions and toxic re-actions that limit their clinical applications.
