The C-Truncated δ-Opioid Receptor Underwent Agonist-Dependent Activation and Desensitization
| Autor: | Qiang Wei, Zhi-Qiang Chi, Jie Chen, Chunhe Wang, Zhijie Cheng, De-He Zhou, Gang Pei, Gui-Fen Li |
|---|---|
| Rok vydání: | 1998 |
| Předmět: |
Agonist
medicine.drug_class medicine.medical_treatment Biophysics CHO Cells Biology Transfection Polymerase Chain Reaction Biochemistry Mice Structure-Activity Relationship Opioid receptor Cricetinae Receptors Opioid delta medicine Animals Staurosporine Enzyme Inhibitors Phosphorylation Receptor Protein Kinase Inhibitors Molecular Biology Desensitization (medicine) Ligand binding assay Chinese hamster ovary cell Cell Membrane Enkephalins Cell Biology Protein kinase inhibitor Molecular biology Peptide Fragments Guanosine 5'-O-(3-Thiotriphosphate) Enkephalin D-Penicillamine (2 5) medicine.drug |
| Zdroj: | Biochemical and Biophysical Research Communications. 249:321-324 |
| ISSN: | 0006-291X |
| DOI: | 10.1006/bbrc.1998.9080 |
| Popis: | The agonist-dependent activation and desensitization of a recombinant analog of delta-opioid receptor lacking the carboxyl-terminal (C-terminal) 31 residue peptide segment were discussed. The cDNA of the C-truncated delta-opioid receptor was created by polymerase chain reaction (PCR), stably expressed in Chinese hamster ovary cells and characterized by binding assay and function assay. Agonist [D-Pen2, D-Pen5]-enkephalin (DPDPE) stimulated the specific [35S]GTPgammaS binding to membrane fragments of cells expressing the C-truncated and the wild-type delta-opioid receptors in different levels dose-dependently. EC50 values of DPDPE on truncated and wild-types in stimulation were very similar. Agonist-dependent desensitization, which could be blocked by protein kinase inhibitor staurosporine (Stau), was observed after pretreating truncated receptors with 1 microM DPDPE for 10 min, the same as wild-types. The results reveal that the C-terminal of the delta-opioid receptor is not involved in controlling the G-protein activation and phosphorylation-related functional desensitization. |
| Databáze: | OpenAIRE |
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