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A fluorescence based reporter construct for the direct detection of TGF-beta receptor activation and modulators thereof

机译:用于直接检测TGF-β受体激活及其调节剂的基于荧光的报告基因构建体

摘要

The invention comprises a fusion protein as sensor for TGF-beta receptor activity, a method for detecting receptor activity and to screening compounds for modulators of receptor activity. The fusion protein comprises a type I TGF-beta receptor, a circularly permutated fluorescent protein moiety (cpFP) and an activation state specific receptor binding domain, binding specifically to either the activated or inactive form of the TGF-beta receptor. An activation specific interaction between the receptor and the activation state specific receptor binding domain modulates the fluorescence of the cpFP inserted in between. Thus, activation of the receptor can be detected directly by a change in fluorescence of the cpFP.
机译:本发明包括作为TGF-β受体活性的传感器的融合蛋白,检测受体活性和筛选用于受体活性调节剂的化合物的方法。融合蛋白包含I型TGF-β受体,环状排列的荧光蛋白部分(cpFP)和活化状态特异性受体结合结构域,其与TGF-β受体的活化或失活形式特异性结合。受体和活化状态特异性受体结合结构域之间的活化特异性相互作用调节插入其间的cpFP的荧光。因此,可以通过cpFP的荧光变化直接检测受体的激活。

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