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Technologies for transporter drug discovery.
Channels ( IF 3.3 ) Pub Date : 2008-11-08 , DOI: 10.4161/chan.2.5.6896
Adam B Weinglass 1 , Maria L Garcia , Gregory L Kaczorowski
Affiliation  

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.

中文翻译:

发现转运蛋白的技术。

转运蛋白是药物发现的有吸引力的靶标,并且涉及哮喘,心血管疾病,糖尿病和神经科学等多个治疗领域的疾病的病理生理学。然而,转运蛋白的内在机械特性对高通量筛选方法的发展提出了重大挑战。这篇综述提供了有关潜在转运蛋白目标的最新信息,并评估了可用技术对转运蛋白的筛选,铅优化和药代动力学评估的影响。
更新日期:2019-11-01
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