Olah Barbara, Tarjanyi Vera, Takacs Barbara, Pluzsnyik Edua, Viczjan Gabor, Ovari Ignac, Szilvassy Zoltan, Juhasz Bela, Zsuga Judit, Erdei Tamas, Gesztelyi Rudolf
Department of Orthodontics, Faculty of Dentistry, University of Debrecen, Debrecen, Hungary.
University of Debrecen, Doctoral School of Nutrition and Food Sciences, Debrecen, Hungary.
Front Pharmacol. 2025 Jun 12;16:1591761. doi: 10.3389/fphar.2025.1591761. eCollection 2025.
The Signal Amplification, Binding affinity, and Receptor-activation Efficacy (SABRE) model is the most recent general and quantitative model of receptor function, which enables the determination of K (the equilibrium dissociation constant of the agonist-receptor complex) and q (the fraction of the operable receptors after a partial irreversible receptor inactivation) from purely functional data. The practical aim of the present study was to test the capabilities of this new model using concentration-effect (E/c) data from a previous investigation conducted in our laboratory. We have found that the SABRE model is at least as useful as two widely accepted older methods thought to have similar capabilities, the operational model of agonism and Furchgott's method, even if the quality of the data to be evaluated is somewhat challenging. Nevertheless, the SABRE model seems to require a large amount of high-quality and, regarding the experimental design, diverse data. In addition, it is important to find the most suitable fitting strategy for the particular sort of data in order to obtain reliable results. However, owing to its unique feature of distinguishing between receptor activation and activation of postreceptorial signaling, the SABRE model appears to be superior to previous quantitative receptor function models in simulating E/c curves and thereby clarifying, explaining or simply illustrating theoretical issues.
信号放大、结合亲和力和受体激活效能（SABRE）模型是受体功能领域最新的通用定量模型，它能够仅从功能数据确定K（激动剂 - 受体复合物的平衡解离常数）和q（部分不可逆受体失活后可操作受体的比例）。本研究的实际目的是利用我们实验室之前一项研究中的浓度 - 效应（E/c）数据来测试这个新模型的能力。我们发现，即使待评估数据的质量颇具挑战性，SABRE模型至少与另外两种被广泛接受且被认为具有类似能力的旧方法——激动作用的操作模型和弗奇戈特方法——同样有用。然而，SABRE模型似乎需要大量高质量且在实验设计方面多样化的数据。此外，为了获得可靠的结果，找到最适合特定类型数据的拟合策略很重要。不过，由于其在区分受体激活和受体后信号激活方面的独特特性，SABRE模型在模拟E/c曲线以及由此阐明、解释或简单说明理论问题方面似乎优于先前的定量受体功能模型。
