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Study of interaction between agonists and Asn293 in Helix VI of human β2-adrenergic receptor

HM Zuurmond, J Hessling, K Blüml, M Lohse…

文献索引:Zuurmond, Helene M.; Hessling, Jutta; Blueml, Klaus; Lohse, Martin; Ijzerman, Adriaan P. Molecular Pharmacology, 1999 , vol. 56, # 5 p. 909 - 916

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被引用次数: 28

摘要

Abstract Previously, we demonstrated the involvement of Asn293 in helix VI of the human β 2-adrenergic receptor in stereoselective agonist recognition and activation. In the present study, we have further explored the role of this residue by synthesizing derivatives of isoproterenol and clenbuterol, two β-adrenergic receptor agonists. We analyzed their efficacy and affinity on the wild-type and a mutant receptor (Asn293Leu). Each compound ...