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Lead compound optimization strategy(8)-drug transporters and related drug design strategies
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Xiao-han SONG1, 2, Jiang WANG1, 2, Hong LIU*, 1, 2
Acta Pharmaceutica Sinica | 2021, 56(2) : 432 - 444
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Acta Pharmaceutica Sinica | 2021, 56(2): 432-444
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Lead compound optimization strategy(8)-drug transporters and related drug design strategies
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Xiao-han SONG1, 2, Jiang WANG1, 2, Hong LIU*, 1, 2
Affiliations
  • 1. State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China
  • 2. University of Chinese Academy of Sciences, Beijing 100049, China
Published: 2021-02-12 doi: 10.16438/j.0513-4870.2020-1248
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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.

transporter  /  drug design  /  lead compound
Xiao-han SONG, Jiang WANG, Hong LIU. Lead compound optimization strategy(8)-drug transporters and related drug design strategies[J]. Acta Pharmaceutica Sinica, 2021 , 56 (2) : 432 -444 . DOI: 10.16438/j.0513-4870.2020-1248
Year 2021 volume 56 Issue 2
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Article Info
doi: 10.16438/j.0513-4870.2020-1248
  • Receive Date:2020-07-27
  • Online Date:2025-12-18
  • Published:2021-02-12
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  • Received:2020-07-27
  • Revised:2020-09-01
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    1. State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China
    2. University of Chinese Academy of Sciences, Beijing 100049, China
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表12种不同金属材料的力学参数

Family
属数
Number of
genus
种数
Number of
species
占总种数比例
Percentage of
total species (%)

Genus
种数
Number of
species
占总种数比例
Percentage of total
species (%)
鹅膏菌科Amanitaceae 2 11 5.26 鹅膏菌属 Amanita 10 4.78
小菇科 Mycenaceae 2 12 5.74 丝盖伞属 Inocybe 5 2.39
多孔菌科 Polyporaceae 8 14 6.70 蜡蘑属 Laccaria 5 2.39
红菇科 Russulaceae 3 23 11.00 小皮伞属 Marasmius 6 2.87
小菇属 Mycena 11 5.26
光柄菇属 Pluteus 5 2.39
红菇属 Russula 17 8.13
栓菌属 Trametes 5 2.39
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