Research progress of P-glycoprotein induction
10.11665/j.issn.1000 -5048.20180104
- VernacularTitle:P-糖蛋白诱导作用的研究进展
- Author:
Yue XU
1
;
Genfu CHEN
;
Tao XIONG
;
Ying PENG
;
Tingting RUAN
;
Guangji WANG
;
Jianguo SUN
Author Information
1. 中国药科大学药物代谢动力学重点实验室
- Keywords:
P-glycoprotein;
induction;
cell model;
antidotal effect
- From:
Journal of China Pharmaceutical University
2018;49(1):26-33
- CountryChina
- Language:Chinese
-
Abstract:
P-glycoprotein(P-gp)is an important efflux protein of ATP-binding cassette transporter superfamily. Cells could be protected from detrimental xenobiotics by the up-regulation of efflux pumps.In this review, an extensive literature search for P-gp induction research was conducted, and a focus was brought onto the P-gp induction models,experiment methods and its applications in drug discovery.We mainly introduced the in vitro cell-based models and in vivo rodent animal models for induction research, methods that investigate induction potency by detecting the protein,gene expression and efflux function,as well as co-regulation between P-gp and other transporters or drug metabolism enzymes.P-gp induction can serve as a clinical therapeutic strategy by reducing the intracellular concentration of deleterious xenobiotics significantly,and the in silico P-gp induction pharmacophore model was also discussed.This review could be of great importance for pre-clinical drug design, the screening of new synthesized compounds and the prediction of potential clinical drug-drug interactions.
