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髓系恶性肿瘤中的激酶抑制剂筛选

Kinase Inhibitor Screening in Myeloid Malignancies.

作者信息

Tyner Jeffrey W

机构信息

Department of Cell, Developmental and Cancer Biology, Knight Cancer Institute, Oregon Health and Science University, OHSU BRB 511, Mailcode L592, 3181 Southwest Sam Jackson Park Road, Portland, OR 97239, USA.

出版信息

Hematol Oncol Clin North Am. 2017 Aug;31(4):693-704. doi: 10.1016/j.hoc.2017.04.004. Epub 2017 May 19.

Abstract

Kinase pathways are primary effectors of many targeted therapy approaches for cancer. Kinase pathways can be dysregulated by mechanisms far more diverse than chromosomal rearrangements or point mutations, which drove the initial application of kinase inhibitors to cancer. Functional screening with kinase inhibitors is one tool by which we can understand the diversity of target kinases and candidate drugs for patients before fully understanding the mechanistic rationale for kinase pathway dysregulation. By combining functional screening with genomic data, it is also possible to accelerate understanding of these mechanistic underpinnings.

摘要

激酶通路是许多癌症靶向治疗方法的主要效应器。激酶通路的失调机制远比染色体重排或点突变多样,而正是这些机制推动了激酶抑制剂在癌症治疗中的最初应用。使用激酶抑制剂进行功能筛选是一种工具,通过它我们可以在充分理解激酶通路失调的机制原理之前,了解患者靶激酶和候选药物的多样性。通过将功能筛选与基因组数据相结合,也有可能加速对这些机制基础的理解。

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