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G 蛋白偶联受体微阵列在药物发现中的应用。

G protein-coupled receptor microarrays for drug discovery.

机构信息

Biochemical Sciences Science and Technology, Division Corning Incorporated, Sullivan Park, Corning, NY 14831, USA.

出版信息

Drug Discov Today. 2004 Dec 15;9(24 Suppl):S61-7.

Abstract

The dominance of G protein-coupled receptors (GPCRs) as a drug target class, coupled with the increased pace of target identification and expansion of compound libraries, presents a compelling need to develop technologies to screen multiple GPCRs simultaneously. To address this need, GPCR microarrays that require the co-immobilization of lipid molecules and the probe receptors of interest have been fabricated, using conventional robotic printing technologies. Assays to screen compounds for their pharmacological properties (binding affinity, relative potency and selectivity) using GPCR microarrays are discussed.

摘要

G 蛋白偶联受体 (GPCRs) 作为药物靶点的主导地位,加上目标识别的步伐加快和化合物库的扩大,迫切需要开发同时筛选多种 GPCR 的技术。为了解决这一需求,已经使用传统的机器人打印技术制造了需要共固定脂质分子和探针受体的 GPCR 微阵列。讨论了使用 GPCR 微阵列筛选化合物的药理学特性(结合亲和力、相对效力和选择性)的测定方法。

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