细胞热转移分析评估细胞内药物靶标相互作用。

The cellular thermal shift assay for evaluating drug target interactions in cells.

机构信息

Department of Medical Biochemistry and Biophysics, Division of Biophysics, Karolinska Institutet, Stockholm, Sweden.

Chemical Biology Consortium Sweden, Science for Life Laboratory Stockholm, Division of Translational Medicine and Chemical Biology, Department of Medical Biochemistry and Biophysics, Karolinska Institutet, Solna, Sweden.

出版信息

Nat Protoc. 2014 Sep;9(9):2100-22. doi: 10.1038/nprot.2014.138. Epub 2014 Aug 7.

Abstract

Thermal shift assays are used to study thermal stabilization of proteins upon ligand binding. Such assays have been used extensively on purified proteins in the drug discovery industry and in academia to detect interactions. Recently, we published a proof-of-principle study describing the implementation of thermal shift assays in a cellular format, which we call the cellular thermal shift assay (CETSA). The method allows studies of target engagement of drug candidates in a cellular context, herein exemplified with experimental data on the human kinases p38α and ERK1/2. The assay involves treatment of cells with a compound of interest, heating to denature and precipitate proteins, cell lysis, and the separation of cell debris and aggregates from the soluble protein fraction. Whereas unbound proteins denature and precipitate at elevated temperatures, ligand-bound proteins remain in solution. We describe two procedures for detecting the stabilized protein in the soluble fraction of the samples. One approach involves sample workup and detection using quantitative western blotting, whereas the second is performed directly in solution and relies on the induced proximity of two target-directed antibodies upon binding to soluble protein. The latter protocol has been optimized to allow an increased throughput, as potential applications require large numbers of samples. Both approaches can be completed in a day.

摘要

热转移分析用于研究配体结合对蛋白质热稳定性的影响。这种分析方法在药物发现行业和学术界中被广泛应用于纯化蛋白质,以检测相互作用。最近,我们发表了一项原理验证研究,描述了在细胞形式中实施热转移分析的方法,我们称之为细胞热转移分析(CETSA)。该方法允许在细胞环境中研究候选药物的靶标结合,本文以人类激酶 p38α 和 ERK1/2 的实验数据为例。该测定法涉及用感兴趣的化合物处理细胞,加热使蛋白质变性沉淀,细胞裂解,以及将细胞碎片和聚集体与可溶性蛋白质部分分离。未结合的蛋白质在高温下变性沉淀,而与配体结合的蛋白质则保持在溶液中。我们描述了两种检测样品可溶性部分中稳定蛋白质的方法。一种方法涉及使用定量 Western blot 进行样品处理和检测,而另一种方法则直接在溶液中进行,依赖于两个靶向目标的抗体在结合可溶性蛋白时的接近程度。后一种方案已被优化以提高通量,因为潜在的应用需要大量的样品。这两种方法都可以在一天内完成。

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