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早期药物发现中的激酶谱分析:理清头绪。

Kinase profiling in early stage drug discovery: sorting things out.

作者信息

Defert Olivier, Boland Sandro

机构信息

Amakem Therapeutics N.V. Agoralaan Abis, 3590 Diepenbeek, Belgium.

Amakem Therapeutics N.V. Agoralaan Abis, 3590 Diepenbeek, Belgium.

出版信息

Drug Discov Today Technol. 2015 Nov;18:52-61. doi: 10.1016/j.ddtec.2015.10.002. Epub 2015 Nov 18.

DOI:10.1016/j.ddtec.2015.10.002
PMID:26723893
Abstract

Protein kinases represent one of the largest superfamilies of drugable targets and a major research area for both the pharmaceutical industry and academic groups. This has resulted in the emergence of numerous screening technologies and services dedicated to kinase profiling. In spite of this plentiful offering, the field is not without its own pitfalls, as the profusion of reported conditions and data can ultimately complicate interpretation of project results. Here, we discuss how kinase profiling was used in our early stage drug discovery efforts, from the perspective of a smaller biotech relying largely on assay outsourcing.

摘要

蛋白激酶是可成药靶点中最大的超家族之一,也是制药行业和学术团体的主要研究领域。这导致了众多致力于激酶谱分析的筛选技术和服务的出现。尽管有如此丰富的资源,但该领域并非没有自身的陷阱,因为大量报道的条件和数据最终可能会使项目结果的解读变得复杂。在此,我们将从一个主要依赖检测外包的小型生物技术公司的角度,讨论激酶谱分析在我们早期药物发现工作中的应用。

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1
Kinase profiling in early stage drug discovery: sorting things out.早期药物发现中的激酶谱分析:理清头绪。
Drug Discov Today Technol. 2015 Nov;18:52-61. doi: 10.1016/j.ddtec.2015.10.002. Epub 2015 Nov 18.
2
Protein kinase profiling assays: a technology review.蛋白激酶分析检测:技术综述
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Bacterial histidine kinases as novel antibacterial drug targets.细菌组氨酸激酶作为新型抗菌药物靶点
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Pocketome of human kinases: prioritizing the ATP binding sites of (yet) untapped protein kinases for drug discovery.人类激酶口袋组学:优先考虑(尚未)开发的蛋白激酶的 ATP 结合位点,以用于药物发现。
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A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.支持激酶信号研究和药物发现的化学基因组图谱的广泛活性屏幕。
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Unexpected off-targets and paradoxical pathway activation by kinase inhibitors.激酶抑制剂引发的意外脱靶效应和矛盾的信号通路激活。
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