G-protein-coupled receptors are one of the most important protein superfamilies as drug targets in drug discovery programs. Their interactions with ligands are influenced by their homomerization. In this study, we propose an operational model for receptor homodimers, which includes constitutive receptor activity. Distinct functional response curves can be obtained from this model, which can satisfactorily depict typical complex experimental data as biphasic and bell-shaped curves. Operational parameters in the model can provide mechanistic explanations for observed functional complexity associated with the cooperativity and intrinsic efficacy of ligands. Because the model presented here is derived from the conceptual framework of operational models, it takes advantage of the body of knowledge coming from the widespread use of this type of modeling. The operational homodimer model can also explain the biased signaling dependent on ligand concentration. In conclusion, this operational homodimer model has a wide range of applications in pharmacological research.

G蛋白偶联受体是最重要的蛋白质超家族之一，在药物开发计划中作为药物靶标。它们与配体的相互作用受其均化作用的影响。在这项研究中，我们提出了一种受体同型二聚体的操作模型，其中包括组成型受体活性。可以从该模型获得不同的功能响应曲线，该曲线可以令人满意地将典型的复杂实验数据描绘为双相和钟形曲线。该模型中的操作参数可以为观察到的与配体的协同作用和内在功效相关的功能复杂性提供机械解释。由于此处介绍的模型是从操作模型的概念框架派生而来的，因此它利用了来自广泛使用这种模型的知识。操作同二聚体模型也可以解释依赖于配体浓度的偏向信号。总之，这种操作性同二聚体模型在药理研究中具有广泛的应用。