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Quantifying the allosteric interactions within a G-protein-coupled receptor heterodimer
Drug Discovery Today ( IF 6.5 ) Pub Date : 2017-07-27 , DOI: 10.1016/j.drudis.2017.07.009
Bin Zhou , Jesús Giraldo

G-protein-coupled receptors are central to signal transduction and cell communication. The possibility that cells use receptor heteromerization to modulate individual receptor pathways is a surmise that cannot be precluded. Given the complexity of these processes, mathematical models contribute to understanding how receptors and their respective ligands regulate signaling. Here, a mathematical model is presented that quantifies the allosteric interactions within a receptor heterodimer. The model is based on the operational model of allosterism including constitutive receptor activity, which provides the pharmacological analysis of heteromerization with well-established and widely used modeling and fitting procedures.



中文翻译:

量化G蛋白偶联受体异二聚体中的变构相互作用

G蛋白偶联受体对于信号转导和细胞通讯至关重要。细胞利用受体异源性调节单个受体途径的可能性是无法排除的。考虑到这些过程的复杂性,数学模型有助于理解受体及其各自的配体如何调节信号传导。在这里,提出了一个数学模型,该模型量化了受体异二聚体中的变构相互作用。该模型基于包括组成型受体活性在内的变构作用的操作模型,该模型通过已建立且广泛使用的建模和拟合程序提供了异源化的药理学分析。

更新日期:2017-07-27
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