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A2 腺苷受体的激活机制。II. 受体 - 效应器相互作用的受限碰撞偶联模型。

Mechanism of activation of A2 adenosine receptors. II. A restricted collision-coupling model of receptor-effector interaction.

作者信息

Gross W, Lohse M J

机构信息

Pharmakologisches Institut, Universität Heidelberg, FRG.

出版信息

Mol Pharmacol. 1991 Apr;39(4):524-30.

PMID:2017152
Abstract

Existing models describing the kinetics of receptor-effector interaction were found to be insufficient to account for the experimental findings on adenylate cyclase activation by A2 adenosine receptors described in the preceding manuscript [Mol. Pharmacol. 39: 517-523 (1991)]. We have, therefore, chosen another approach and have developed discrete computer simulations of receptor-effector interactions taking place on a spherical membrane. These simulations were based on the following principles: (a) receptors activate effectors in a catalytic manner, and (b) diffusion of receptors and effectors is slow, so that receptors will only activate effectors that are in their vicinity at the time of agonist occupation. Using several experimentally determined parameters, these simulations could reproduce the experimental findings on adenylate cyclase activation by A2 adenosine receptors described in the preceding manuscript. In addition, by appropriate choice of the simulation parameters, they are shown to accommodate the behavior of several other models of receptor-effector interactions.

摘要

已发现现有的描述受体 - 效应器相互作用动力学的模型不足以解释前文手稿[《分子药理学》39: 517 - 523 (1991)]中所述的A2腺苷受体激活腺苷酸环化酶的实验结果。因此,我们选择了另一种方法,并开发了在球形膜上发生的受体 - 效应器相互作用的离散计算机模拟。这些模拟基于以下原则:(a) 受体以催化方式激活效应器,以及(b) 受体和效应器的扩散缓慢,因此在激动剂占据时,受体只会激活其附近的效应器。使用几个实验确定的参数,这些模拟能够重现前文手稿中所述的A2腺苷受体激活腺苷酸环化酶的实验结果。此外,通过适当选择模拟参数,它们被证明能够适应其他几种受体 - 效应器相互作用模型的行为。

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