Modelling of signalling via G-protein coupled receptors: Pathway-dependent agonist potency and efficacy
Modelling of signalling via G-protein coupled receptors: Pathway-dependent agonist potency and efficacy
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DOI：
10.1016/s0092-8240(03)00055-7
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发表时间：
2003-09-01
影响因子：
3.5
通讯作者：
King, JR
中科院分区：
文献类型：
--
作者：
Chen, CY;Cordeaux, Y;King, JR
构建了一个数学模型来研究受体与G蛋白的混杂偶联，并模拟导致细胞内多个效应通路激活的事件。该模型旨在更好地理解决定药物疗效和效力的因素。假设受体可以存在于多个构象状态，并允许激动剂的具体构象，构建一个系统的常微分方程，并随后的途径依赖性激动剂的效力和效力顺序进行预测。还给出了一个简单的情况下的受体和G-蛋白的区室化，使用当前的模型来说明空间异质性对预测响应的影响。(C)2003 Society for Mathematical Biology由Elsevier Ltd.出版，版权所有。
A mathematical model is constructed to study promiscuous coupling of receptors to G-proteins and to simulate events leading to the activation of multiple effector pathways within a cell. The model is directed at a better understanding of the factors that determine the efficacy and potency of a drug. Assuming that the receptors can exist in multiple conformational states, and allowing for agonist specific conformation, a system of ordinary differential equations is constructed and subsequently pathway-dependent agonist efficacy and potency order is predicted. A simple case of the compartmentalization of receptors and G-proteins is also given, using the current model to illustrate the effects of spatial heterogeneity on the predicted response. (C) 2003 Society for Mathematical Biology Published by Elsevier Ltd. All rights reserved.