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首页> 外文期刊>Neurochemistry International: The International Journal for the Rapid Publication of Critical Reviews, Preliminary and Original Research Communications in Neurochemistry >Kinetic versus allosteric mechanisms to explain insurmountable antagonism and delayed ligand dissociation.
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Kinetic versus allosteric mechanisms to explain insurmountable antagonism and delayed ligand dissociation.

机译：动力学和变构机制来解释不可克服的拮抗作用和延迟的配体解离。

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摘要

The present review addresses the theories which have been advanced to explain experimental observations dealing with insurmountable antagonism and accelerated radioligand dissociation in the presence of an excess unlabelled ligand. We came to the perception that, for each of these phenomena, the theories can be placed into two distinctive categories. The "kinetic" interpretations attribute these phenomena to, respectively, the ability of antagonists to form long-lasting complexes with their cognate receptor and the ability of dissociated ligands to bind again to the same or neighbouring receptors rather than to diffuse away from the cell surface. On the other hand, these observations can also be explained by negative allosteric interactions among topographically distinct ligand binding sites at the same receptor or di/multimeric receptor complex.
机译：本综述解决了已经提出的理论，以解释在过量的未标记配体存在下无法克服的拮抗作用和加速放射性配体解离的实验观察。我们意识到，对于每种现象，理论都可以分为两个不同的类别。 “动力学”的解释将这些现象分别归因于拮抗剂与其同源受体形成持久复合物的能力，以及解离的配体再次结合至相同或邻近受体而不是扩散离开细胞表面的能力。 。另一方面，这些观察结果也可以通过在相同受体或二/多聚体受体复合物上形貌独特的配体结合位点之间的负变构相互作用来解释。

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