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Similar apparent constitutive activity of human histamine H_2-receptor fused to long and short splice variants of Gsa,

Wenzel-Seifert, Katharina ; Kelley, Melissa T. ; Buschauer, Armin ; Seifert, Roland



Abstract

Fusion proteins allow for the analysis of receptor/G protein coupling under defined conditions. The beta 2-adrenoceptor (beta 2AR) fused to the long splice variant of Gsalpha (Gsalpha L) exhibits a higher apparent constitutive activity than the beta 2-adrenoceptor fused to the short splice variant of Gsalpha (Gsalpha S). Experimentally, this results in higher efficacy and potency of partial ...

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