Physical characterization of native opiate receptors. Additional information from detailed binding analysis of a radiation-inactivated receptor.
Physical characterization of native opiate receptors. Additional information from detailed binding analysis of a radiation-inactivated receptor.
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天然阿片受体的物理特征。
DOI：
10.1016/0167-4889(87)90032-2
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发表时间：
1987
期刊：
影响因子：
--
通讯作者：
Glasel,JA
中科院分区：
文献类型：
--
作者：
Glasel,JA
用放射灭活技术对冷冻的大鼠脑匀浆进行了依托吗啡受体的靶向大小分析。在每个辐射剂量下的多点饱和曲线表明，该配体与其受体结合的表观解离常数是剂量的函数。对结果的分析清楚地表明，配体结合的大分子至少与另一个大分子功能偶联。当偶合作用被破坏时，配体的离解常数变大一个数量级以上。因此，解离常数随剂量的变化产生了关于天然受体性质的有趣的新信息，这对于结合部位的构象以及针对阿片受体配体结合成分测序的增溶和克隆方法具有重要意义。
Target size analyses of the etorphine receptor were performed on frozen rat brain P2homogenates using the radiation inactivation technique. Multi-point saturation curves at each radiation dose revealed that the apparent dissociation constant for the binding of this ligand to its receptor is a function of the dose. Analysis of the results shows clearly that the ligand-binding macromolecule is functionally coupled to at least one other macromolecule. When the coupling is destroyed the ligand dissociation constant becomes larger by over an order of magnitude. Thus, the variation of the dissociation constant with dose yields interesting new information on the nature of the native receptor which has implications with respect to the conformation of the binding site and to solubilization and cloning methods directed towards sequencing the ligand-binding component of opiate receptors.