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.

S Swillens
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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.

活化β -肾上腺素能受体数量对腺苷酸环化酶儿茶酚胺活化的调节:细胞膜中受体扩散作用的理论考虑。
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有关。在S49淋巴瘤细胞中,先前已经表明,对于给定数量的占据受体,腺苷酸环化酶活性水平取决于受体的总数。在这里,我们提出并证明,这种行为可以用Cassel和Selinger的循环模型来解释,只要受体在膜平面上的扩散在模型中被明确地引入。这个扩展版模型的关键特性与受体扩散和受体激动剂解离的相对动力学有关。
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