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高通量亲和选择质谱在药物发现中用于筛选化学化合物文库的应用。

Application of high-throughput affinity-selection mass spectrometry for screening of chemical compound libraries in lead discovery.

机构信息

Novartis Institutes for BioMedical Research.

出版信息

Expert Opin Drug Discov. 2007 Feb;2(2):285-94. doi: 10.1517/17460441.2.2.285.

DOI:10.1517/17460441.2.2.285
PMID:23496083
Abstract

High-throughput screening of chemical libraries for compounds that interfere with a particular molecular target is among the most powerful methodologies applied in lead discovery at present. In this review, the authors describe a label-free, homogeneous, affinity-selection-based technology developed at Novartis, termed SpeedScreen, which is compared with similar technologies used for high-throughput screening in the pharmaceutical and biotechnology industries. The focus at present of SpeedScreen is twofold: first, this technology is applied to orphan genomic targets and to those targets that are non-tractable by a functional assay; second, this technology is applied complementary to the well-established traditional methodologies for the screening of molecular targets. In summary, the authors discuss the value of affinity-selection-based high-throughput screening as a complementary technology to the common functional screening platforms and the benefits as well as the limitations of this new technology are outlined.

摘要

高通量筛选化学文库中干扰特定分子靶标的化合物是目前在先导化合物发现中应用最广泛的方法之一。在这篇综述中,作者描述了一种由诺华公司开发的无标记、均相、基于亲和选择的技术,称为 SpeedScreen,并将其与制药和生物技术行业中用于高通量筛选的类似技术进行了比较。目前,SpeedScreen 的重点有两个方面:首先,该技术应用于孤儿基因组靶标和那些无法通过功能测定的靶标;其次,该技术作为对成熟的传统分子靶标筛选方法的补充。总之,作者讨论了基于亲和选择的高通量筛选作为对常见功能筛选平台的补充技术的价值,以及概述了这项新技术的优势和局限性。

相似文献

1
Application of high-throughput affinity-selection mass spectrometry for screening of chemical compound libraries in lead discovery.高通量亲和选择质谱在药物发现中用于筛选化学化合物文库的应用。
Expert Opin Drug Discov. 2007 Feb;2(2):285-94. doi: 10.1517/17460441.2.2.285.
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A chemoinformatics analysis of hit lists obtained from high-throughput affinity-selection screening.对通过高通量亲和筛选获得的命中列表进行的化学信息学分析。
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Novel trends in high-throughput screening.高通量筛选的新趋势。
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Affinity-based screening techniques: their impact and benefit to increase the number of high quality leads.基于亲和力的筛选技术:其对增加高质量先导化合物数量的影响和益处。
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SpeedScreen: The "missing link" between genomics and lead discovery.SpeedScreen:基因组学与先导化合物发现之间的“缺失环节”。
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Tackling the chemogenomic space by novel screening technologies.通过新型筛选技术攻克化学基因组学领域。
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SpeedScreen: label-free liquid chromatography-mass spectrometry-based high-throughput screening for the discovery of orphan protein ligands.快速筛选:基于无标记液相色谱-质谱联用的高通量筛选技术,用于发现孤儿蛋白配体。
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Discovery and characterization of orthosteric and allosteric muscarinic M2 acetylcholine receptor ligands by affinity selection-mass spectrometry.通过亲和选择质谱法发现并表征正构和变构毒蕈碱M2型乙酰胆碱受体配体
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Label-free screening assays: a strategy for finding better drug candidates.无标记筛选检测法:寻找更好药物候选物的策略。
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