C端截短的δ阿片受体的结合特性
Binding properties of C-truncated delta opioid receptors.
作者信息
Wang C H, Zhou D H, Chen J, Li G E, Pei G, Chi Z Q
机构信息
Shanghai Institute of Materia Medica, Chinese Academy of Sciences, China.
出版信息
Zhongguo Yao Li Xue Bao. 1997 Jul;18(4):337-40.
AIM
To study the role of C-terminal delta opioid receptor involved in ligand binding affinity and selectivity.
METHODS
The 31 amino acid residues of C-terminal truncated delta opioid receptors and the wild-type were expressed stably in Chinese hamster ovary (CHO) cells, respectively. Then the ligand binding properties of the products were studied by receptor binding assay.
RESULTS
A typical mutated receptor clone CHO-T and a wild-type receptor clone CHO-W were obtained. The Kd values of [3H] diprenorphine (Dip) and [3H]leucine-2-alanine enkephalin (DADLE) bound to CHO-T were similar to CHO-W. Both the specific [3H]Dip bindings of CHO-T and CHO-W were strongly inhibited by delta selective agonists with similar Ki, but neither by mu nor kappa selective agonists.
CONCLUSION
The C-terminal of the delta opioid receptor is not involved in the ligands binding affinity and selectivity.
目的
研究δ阿片受体C末端在配体结合亲和力和选择性中的作用。
方法
将C末端截短的δ阿片受体的31个氨基酸残基和野生型分别在中国仓鼠卵巢（CHO）细胞中稳定表达。然后通过受体结合试验研究产物的配体结合特性。
结果
获得了一个典型的突变受体克隆CHO-T和一个野生型受体克隆CHO-W。与CHO-T结合的[3H]二丙诺啡（Dip）和[3H]亮氨酸-2-丙氨酸脑啡肽（DADLE）的Kd值与CHO-W相似。CHO-T和CHO-W的特异性[3H]Dip结合均被具有相似Ki的δ选择性激动剂强烈抑制，但未被μ或κ选择性激动剂抑制。
结论
δ阿片受体的C末端不参与配体结合亲和力和选择性。
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