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Binding properties of C-truncated delta opioid receptors
1Shanghai Institute of Materia Medica, Chinese Academy of Sciences, China.
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.
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