Topological Polar Surface Area Defines Substrate Transport by Multidrug Resistance Associated Protein 1 (MRP1/ABCC1)

被引：86

作者：

Fernandes, Janaina ^{[1
]}

Gattass, Cerli R. ^{[1
]}

机构：

[1] Univ Fed Rio de Janeiro, Inst Biofis Carlos Chagas Filho, Ctr Ciencias Saude, Lab Imunol Celular, BR-21949900 Rio De Janeiro, Brazil

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2009年 / 52卷 / 04期

关键词：

GLUTATHIONE-S-TRANSFERASE; MEDIATED VINCRISTINE RESISTANCE; ATP-DEPENDENT EFFLUX; LEUKOTRIENE C-4; P-GLYCOPROTEIN; MRP1; CONJUGATE; INHIBITION; DRUGS; DETOXIFICATION;

D O I：

10.1021/jm801389m

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Multidrug resistance-associated protein 1 (MRP1/ABCC1) is a very promiscuous transporter. Herein we used topological polar surface area (TPSA), a descriptor defined as the sum of surfaces of polar atoms in a molecule, to analyze drug transport by MRP1. We suggested that compounds with high TPSA are transported while those with low TPSA are not. The conjugation to GSH increases TPSA values favoring transport. A strong correlation between TPSA and transport properties (K-m) was also found.

引用

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页码：1214 / 1218

页数：5

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