Internalization of the rat AT1a and AT1b receptors: pharmacological and functional requirements
| Autor: | Eric Clauser, Catherine Monnot, Pierre Corvol, Betty Teutsch, Sophie Conchon |
|---|---|
| Jazyk: | angličtina |
| Předmět: |
Agonist
medicine.medical_specialty Angiotensin receptor medicine.drug_class media_common.quotation_subject education Biophysics Tetrazoles CHO Cells Biology Biochemistry Losartan Angiotensin Receptor Antagonists Structural Biology Internal medicine Cricetinae Genetics medicine Animals Internalization Receptor Molecular Biology media_common G protein-coupled receptor Angiotensin II receptor type 1 Receptors Angiotensin Dose-Response Relationship Drug Angiotensin II Biphenyl Compounds Antagonist Imidazoles Biological Transport Cell Biology Recombinant Proteins Cell biology Rats Endocrinology G-protein coupled receptor hormones hormone substitutes and hormone antagonists |
| Zdroj: | FEBS Letters. (3):365-370 |
| ISSN: | 0014-5793 |
| DOI: | 10.1016/0014-5793(94)00703-9 |
| Popis: | The capacity of the angiotensin II (AngII) agonist [Sar1]AngII, the antagonist [Sar1-I1e8]AngII and the non-peptidic antagonist DuP753 to undergo receptor internalization were studied in Chinese hamster ovary cells expressing rat AngII type 1a or 1b receptors (AT1a or AT1b) or a mutant of AT1a (Asn74) unable to couple G-protein. In this expression system, the ligand-induced internalization of rat AT1a and AT1b are similar. Moreover, peptidic ligands, either the agonist or antagonist, induce a significant internalization of AT1 receptors, but the non-peptidic antagonist DuP753 is far less potent. Finally, the normal internalization of the mutant Asn74 demonstrates that receptor activation and G-protein coupling are not required for AT1ainternalization. |
| Databáze: | OpenAIRE |
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