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活性β-肾上腺素能受体数量对儿茶酚胺激活腺苷酸环化酶的调节作用:关于受体在细胞膜中扩散作用的理论思考

Modulation of catecholamine activation of adenylate cyclase by the number of active beta-adrenergic receptors: theoretical considerations on the role of receptor diffusion in the cell membrane.

作者信息

Swillens S

出版信息

J Cyclic Nucleotide Res. 1982;8(2):71-82.

PMID:6294157
Abstract

Numerous experimental studies on the beta-adrenergic receptor suggested that the adenylate cyclase activity is correlated to the number of agonist-receptor complexes. In S49 lymphoma cells, it has been previously shown that, for a given number of occupied receptors, the level of adenylate cyclase activity depends on the total number of receptors. Here we propose and demonstrate that such a behaviour can be accounted for by the cyclic model of Cassel and Selinger provided the diffusion of the receptor in the plane of the membrane is explicitly introduced in the model. The key properties of this expanded version of the model are related to the relative kinetics of receptor diffusion and of agonist dissociation from the receptor.

摘要

大量关于β-肾上腺素能受体的实验研究表明,腺苷酸环化酶活性与激动剂-受体复合物的数量相关。在S49淋巴瘤细胞中,先前已经表明,对于给定数量的被占据受体,腺苷酸环化酶活性水平取决于受体的总数。在此我们提出并证明,只要在模型中明确引入受体在膜平面内的扩散,卡塞尔和塞林格的循环模型就能解释这种行为。该模型扩展版本的关键特性与受体扩散和激动剂从受体解离的相对动力学有关。

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