Lead compound optimization strategy (8) - drug transporters and related drug design strategies
10.16438/j.0513-4870.2020-1248
- VernacularTitle:先导化合物结构优化策略 (八) —— 药物转运体及其相关药物设计策略
- Author:
Xiao-han SONG
1
;
Jiang WANG
1
;
Hong LIU
1
Author Information
1. State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China; University of Chinese Academy of Sciences, Beijing 100049, China
- Publication Type:Research Article
- Keywords:
transporter;
rug design;
lead compound
- From:
Acta Pharmaceutica Sinica
2021;56(2):432-444
- CountryChina
- Language:Chinese
-
Abstract:
Transporters have a great influence on the transportation and distribution of drugs in the body. On the one hand, solute carrier transporters could transport drugs into tissues and organs, which may improve the oral bioavailability or change the tissue-distribution of the drugs. On the other hand, the ATP-binding cassette could pump some drugs out of the cell, which decreases the intracellular drug concentrations and leads to drug resistance. This paper summarizes the distribution, substrate characteristics and drug design strategies of several important drug transporters, such as improving bioavailability by prodrug design, introducing acid group to improve hepatic selectivity and adjusting the polarity of compounds to decrease efflux ratio.
