Ins and outs of the ABCG2 multidrug transporter: An update on in vitro functional assays

被引：47

作者：

Hegedus, Csilla ^{[1
,2
]}

Szakacs, Gergely ^{[3
]}

Homolya, Laszlo ^{[1
,2
]}

Orban, Tamas I. ^{[1
,2
]}

Telbisz, Agnes ^{[1
,2
]}

Jani, Marton ^{[4
]}

Sarkadi, Balazs ^{[1
,2
]}

机构：

[1] Semmelweis Univ, Hungarian Acad Sci, Membrane Res Grp, H-1085 Budapest, Hungary

[2] Natl Blood Ctr, Budapest, Hungary

[3] Hungarian Acad Sci, Inst Enzymol, Budapest, Hungary

[4] SOLVO Biotechnol, Budapest, Hungary

来源：

ADVANCED DRUG DELIVERY REVIEWS | 2009年 / 61卷 / 01期

关键词：

ABCG2; Multidrug resistance; ADME-Tox; Membrane-based assays; Cellular assays; Conformation sensitive antibody; Fluorescent proteins; BREAST-CANCER RESISTANCE; CACO-2 CELL MONOLAYERS; PLASMA-MEMBRANE VESICLES; N-LINKED GLYCOSYLATION; HAMSTER OVARY CELLS; HUMAN-TUMOR-CELLS; P-GLYCOPROTEIN; MONOCLONAL-ANTIBODY; PROTEIN BCRP/ABCG2; ATP HYDROLYSIS;

D O I：

10.1016/j.addr.2008.09.007

中图分类号：

R9 [药学];

学科分类号：

100702 [药剂学];

摘要：

The major aim of this chapter is to provide a critical overview of the in vitro methods available for studying the function of the ABCC2 multidrug transporter protein. When describing the most applicable assay systems, in each case we present a short overview relevant to ABC multidrug transporters in general, and then we concentrate on the tools applicable to analysis of substrate-drug interactions, the effects of potential activators and inhibitors, and the role of polymorphisms of the ABCG2 transporter. Throughout this chapter we focus on recently developed assay systems, which may provide new possibilities for analyzing the pharmacological aspects of this medically important protein. (C) 2008 Elsevier B.V. All rights reserved.

引用

页码：47 / 56

页数：10

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