Binding properties of C-truncated delta opioid receptors
Abstract
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.
Keywords:
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.