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不同亚型的阿片受体对G蛋白具有不同的亲和力。

Different subtypes of opioid receptors have different affinities for G-proteins.

作者信息

Polastron J, Jauzac P

机构信息

Laboratoire de Neurosciences, CNRS URA 1829, Caen, France.

出版信息

Cell Mol Biol (Noisy-le-grand). 1994 May;40(3):389-401.

PMID:7920183
Abstract

In this work, we have characterized the opioid receptor expressed by the human neuroblastoma cell line SK-N-BE and compared its hydrodynamic behaviour with those of well known opioid receptors: mu-opioid receptor of rabbit cerebellum and delta-opioid receptor of the hybrid cell line NG 108-15. Human neuroblastoma cell line SK-N-BE expresses a substantial amount of opioid receptors (200-300 fmoles/mg of protein). Pharmacological characterization suggests an heterogenous population of receptors and the presence of two delta subtypes which are, at least partially, negatively coupled with adenylate cyclase via a Gi protein. These receptors exist under two different molecular forms and, in this respect, strikingly contrast with the archetypic delta receptors of NG 108-15 hybrid cell line which show only a high molecular weight form and appear more tightly coupled with the G protein. Hydrodynamic behaviour of SK-N-BE opioid receptors is reminiscent of the profile observed with the rabbit cerebellum mu-opioid receptor. This observation is consistent with the presence of two delta-opioid receptors subtypes, one of which exhibiting properties close to those of mu opioid receptors. Taken overall, our results suggest that different types and subtypes of opioid receptors, even if they are coupled to the same inhibitory G protein, are more or less tightly coupled with their transduction proteins and that closely related opioid receptors can form allosterically interacting complexes.

摘要

在本研究中,我们已对人神经母细胞瘤细胞系SK-N-BE所表达的阿片受体进行了特性鉴定,并将其流体动力学行为与那些已知的阿片受体进行了比较:兔小脑的μ-阿片受体和杂交细胞系NG 108-15的δ-阿片受体。人神经母细胞瘤细胞系SK-N-BE表达大量的阿片受体(200 - 300飞摩尔/毫克蛋白质)。药理学特性表明存在受体的异质群体以及两种δ亚型,它们至少部分地通过Gi蛋白与腺苷酸环化酶负性偶联。这些受体以两种不同的分子形式存在,在这方面,与NG 108-15杂交细胞系的典型δ受体形成鲜明对比,后者仅显示高分子量形式,并且似乎与G蛋白的偶联更紧密。SK-N-BE阿片受体的流体动力学行为让人联想到兔小脑μ-阿片受体所观察到的特征。这一观察结果与存在两种δ-阿片受体亚型一致,其中一种表现出与μ-阿片受体相近的特性。总体而言,我们的结果表明,即使阿片受体的不同类型和亚型与同一抑制性G蛋白偶联,它们与转导蛋白的偶联程度也或多或少有所不同,并且密切相关的阿片受体可以形成变构相互作用复合物。

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Different subtypes of opioid receptors have different affinities for G-proteins.不同亚型的阿片受体对G蛋白具有不同的亲和力。
Cell Mol Biol (Noisy-le-grand). 1994 May;40(3):389-401.
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