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精准靶向激酶。

Targeting kinases with precision.

作者信息

Gardino Alexandra K, Evans Erica K, Kim Joseph L, Brooijmans Natasja, Hodous Brian L, Wolf Beni, Lengauer Christoph

机构信息

Blueprint Medicines, Cambridge, MA, USA.

Accent Therapeutics, Cambridge, MA, USA.

出版信息

Mol Cell Oncol. 2018 Apr 11;5(3):e1435183. doi: 10.1080/23723556.2018.1435183. eCollection 2018.

Abstract

Cancer genomics and mechanistic studies have revealed that heterogeneous mutations within a single kinase can result in a variety of activation mechanisms. The challenge has been to match these insights with tailored drug discovery strategies to yield potent, highly selective drugs. With optimized drugs in hand, physicians could apply the principles of personalized medicine with an increasing number of options to treat patients with improved precision according to their tumor's molecular genotype.

摘要

癌症基因组学和机制研究表明,单一激酶内的异质性突变可导致多种激活机制。挑战在于将这些见解与量身定制的药物发现策略相匹配,以产生强效、高选择性的药物。有了优化后的药物,医生可以应用个性化医疗原则,根据患者肿瘤的分子基因型,有越来越多的选择来更精准地治疗患者。

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本文引用的文献

1
A precision therapy against cancers driven by mutations.
Sci Transl Med. 2017 Nov 1;9(414). doi: 10.1126/scitranslmed.aao1690.
2
AACR Project GENIE: Powering Precision Medicine through an International Consortium.
Cancer Discov. 2017 Aug;7(8):818-831. doi: 10.1158/2159-8290.CD-17-0151. Epub 2017 Jun 1.
3
4
The cBio cancer genomics portal: an open platform for exploring multidimensional cancer genomics data.
Cancer Discov. 2012 May;2(5):401-4. doi: 10.1158/2159-8290.CD-12-0095.
5
The GIST paradigm: lessons for other kinase-driven cancers.
J Pathol. 2011 Jan;223(2):251-61. doi: 10.1002/path.2798. Epub 2010 Oct 26.
6
KIT kinase mutants show unique mechanisms of drug resistance to imatinib and sunitinib in gastrointestinal stromal tumor patients.
Proc Natl Acad Sci U S A. 2009 Feb 3;106(5):1542-7. doi: 10.1073/pnas.0812413106. Epub 2009 Jan 21.
8
Efficacy and safety of imatinib mesylate in advanced gastrointestinal stromal tumors.
N Engl J Med. 2002 Aug 15;347(7):472-80. doi: 10.1056/NEJMoa020461.

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