Identification of a domain of ETA receptor required for ligand binding. |
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Authors: | M Adachi Y Y Yang A Trzeciak Y Furuichi C Miyamoto |
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Institution: | Department of Molecular Genetics, Nippon Roche Research Center, Kamakura, Japan. |
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Abstract: | Various chimeric ETA and ETB receptors were produced in CHO cells for the elucidation of a specific domain which influences the affinity of the receptor toward BQ-123, a selective ETA antagonist. Replacement of the first extracellular loop domain (B-loop) of the ETA receptor with the corresponding domain of the ETB receptor, reduced the inhibition by BQ-123 drastically, while the replacements of other extracellular domains of ETA did not. By contrast, the introduction of the B-loop of ETA in place of the corresponding domain of the ETB receptor endowed the ETB-based chimeric receptor with a sensitivity to BQ-123. These observations suggest that the B-loop domain of the ETA receptor is involved in ligand binding. |
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