文章：

基于活性的蛋白质谱在癌症生化途径发现中的应用

Activity-based protein profiling for biochemical pathway discovery in cancer

原文发布日期：2010-08-12

DOI: 10.1038/nrc2901

类型: Review Article

开放获取: 否

要点：

1. Activity-based protein profiling (ABPP) facilitates the discovery of deregulated enzymes in cancer.
2. Competitive ABPP yields selective inhibitors for functional characterization of cancer enzymes.
3. ABPP can be integrated with metabolomics to map deregulated enzymatic pathways in cancer.
4. ABPP can be integrated with other proteomic methods to map proteolytic pathways in cancer.
5. ABPP probes can be used to image tumour development in living animals.

要点翻译：

1. 基于活性的蛋白质谱分析（ABPP）有助于发现癌症中失调的酶。
2. 竞争性ABPP可产生选择性抑制剂，用于癌症酶的功能表征。
3. ABPP可与代谢组学整合，以绘制癌症中失调的酶促通路图谱。
4. ABPP可与其他蛋白质组学方法结合，以绘制癌症中的蛋白水解通路图谱。
5. ABPP探针可用于活体动物肿瘤发育的成像。

英文摘要：

Large-scale profiling methods have uncovered numerous gene and protein expression changes that correlate with tumorigenesis. However, determining the relevance of these expression changes and which biochemical pathways they affect has been hindered by our incomplete understanding of the proteome and its myriad functions and modes of regulation. Activity-based profiling platforms enable both the discovery of cancer-relevant enzymes and selective pharmacological probes to perturb and characterize these proteins in tumour cells. When integrated with other large-scale profiling methods, activity-based proteomics can provide insight into the metabolic and signalling pathways that support cancer pathogenesis and illuminate new strategies for disease diagnosis and treatment.

摘要翻译： 

大规模分析方法已揭示与肿瘤发生相关的众多基因和蛋白质表达变化。然而，由于我们对蛋白质组及其复杂功能和调控模式的了解尚不完整，确定这些表达变化的意义及其影响的生化途径一直受到阻碍。基于活性的分析平台不仅能发现与癌症相关的酶，还能提供选择性药理学探针，在肿瘤细胞中干扰和表征这些蛋白质。当与其他大规模分析方法结合时，基于活性的蛋白质组学可深入了解支持癌症发病的代谢和信号通路，并为疾病诊断和治疗提供新策略。

原文链接：

Activity-based protein profiling for biochemical pathway discovery in cancer