Technologies for transporter drug discovery

被引：6

作者：

Weinglass, Adam B. ^{[1
]}

Garcia, Maria L. ^{[1
]}

Kaczorowski, Gregory L. ^{[1
]}

机构：

[1] Merck Res Labs, Dept Ion Channels, Rahway, NJ 07065 USA

来源：

CHANNELS | 2008年 / 2卷 / 05期

关键词：

transporter targets; drug development; functional assays; electrogenic; electroneutral; fluorescence; radioactivity; electrophysiology;

D O I：

10.4161/chan.2.5.6896

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Transporters represent attractive targets for drug discovery and are implicated in the pathophysiology of disorders across several therapeutic areas including asthma, cardiovascular disease, diabetes and neuroscience. However, the intrinsic mechanistic properties of transporters present significant challenges to the development of high-throughput screening methodologies. This review provides an update on potential transporter targets and evaluates the impact of available technologies to enable transporter screening, lead optimization and assessment of pharmacokinetics.

引用

页码：312 / 321

页数：10

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