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New opportunities for kinase drug repurposing and target discovery.激酶药物再利用和靶点发现的新机遇。
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本文引用的文献

1
The target landscape of clinical kinase drugs.临床激酶药物的目标格局。
Science. 2017 Dec 1;358(6367). doi: 10.1126/science.aan4368.
2
Quantitative, Wide-Spectrum Kinase Profiling in Live Cells for Assessing the Effect of Cellular ATP on Target Engagement.在活细胞中进行定量、广谱激酶分析，以评估细胞 ATP 对靶标结合的影响。
Cell Chem Biol. 2018 Feb 15;25(2):206-214.e11. doi: 10.1016/j.chembiol.2017.10.010. Epub 2017 Nov 22.
3
Comprehensive characterization of the Published Kinase Inhibitor Set.全面表征已发表的激酶抑制剂集。
Nat Biotechnol. 2016 Jan;34(1):95-103. doi: 10.1038/nbt.3374. Epub 2015 Oct 26.
4
Optimized chemical proteomics assay for kinase inhibitor profiling.用于激酶抑制剂分析的优化化学蛋白质组学检测方法。
J Proteome Res. 2015 Mar 6;14(3):1574-86. doi: 10.1021/pr5012608. Epub 2015 Feb 20.
5
Ten things you should know about protein kinases: IUPHAR Review 14.关于蛋白激酶你应该了解的十件事：IUPHAR综述14
Br J Pharmacol. 2015 Jun;172(11):2675-700. doi: 10.1111/bph.13096. Epub 2015 Mar 24.
6
Dual kinase-bromodomain inhibitors for rationally designed polypharmacology.双激酶-溴结构域抑制剂用于合理设计的多药理学。
Nat Chem Biol. 2014 Apr;10(4):305-12. doi: 10.1038/nchembio.1471. Epub 2014 Mar 2.
7
Network-based approach identified cell cycle genes as predictor of overall survival in lung adenocarcinoma patients.基于网络的方法鉴定出细胞周期基因作为肺腺癌患者总生存期的预测因子。
Lung Cancer. 2013 Apr;80(1):91-8. doi: 10.1016/j.lungcan.2012.12.022. Epub 2013 Jan 26.
8
Cabozantinib (XL184), a novel MET and VEGFR2 inhibitor, simultaneously suppresses metastasis, angiogenesis, and tumor growth.卡博替尼（XL184），一种新型的 MET 和 VEGFR2 抑制剂，可同时抑制转移、血管生成和肿瘤生长。
Mol Cancer Ther. 2011 Dec;10(12):2298-308. doi: 10.1158/1535-7163.MCT-11-0264. Epub 2011 Sep 16.
9
A quantitative analysis of kinase inhibitor selectivity.激酶抑制剂选择性的定量分析。
Nat Biotechnol. 2008 Jan;26(1):127-32. doi: 10.1038/nbt1358.
10
A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.已验证的激酶抑制剂与丝氨酸/苏氨酸激酶的系统性相互作用图谱。
Proc Natl Acad Sci U S A. 2007 Dec 18;104(51):20523-8. doi: 10.1073/pnas.0708800104. Epub 2007 Dec 11.

激酶药物再利用和靶点发现的新机遇。

New opportunities for kinase drug repurposing and target discovery.

机构信息

Institute for Pharmaceutical Chemistry, Johann Wolfgang Goethe-University, Max-von-Laue-Str. 9, Frankfurt, D-60438, Germany.

Structural Genomics Consortium, Buchmann Institute for Molecular Life Sciences, Johann Wolfgang Goethe-University, Max-von-Laue-Str. 15, Frankfurt, D-60438, Germany.

出版信息

Br J Cancer. 2018 Apr;118(7):936-937. doi: 10.1038/s41416-018-0045-6. Epub 2018 Mar 16.

DOI:10.1038/s41416-018-0045-6
PMID:29545596
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC5931101/
Abstract

Protein kinases are major drug targets for oncology. The large size of the kinome, active site conservation and the influence of activation states on drug binding complicates the analysis of their cellular mode of action. In a recent article in Science, Klaeger et al. analysed cellular targets of 243 drug candidates providing a large repository of data for drug repurposing.

摘要

蛋白激酶是肿瘤学的主要药物靶点。激酶组的庞大规模、活性位点的保守性以及激活状态对药物结合的影响，使得分析其细胞作用模式变得复杂。在最近的《科学》杂志的一篇文章中，Klaeger 等人分析了 243 种候选药物的细胞靶标，为药物再利用提供了大量数据存储库。