Article
Allosteric modulation and constitutive activity of fusion proteins between the adenosine A1 receptor and different 351Cys-mutated Gi alpha-subunits.
European journal of pharmacology - 19 Sept 2004
Klaasse Elisabeth, de Ligt Rianne A F, Roerink Sophie F, Lorenzen Anna, Milligan Graeme, Leurs Rob, IJzerman Ad P
Abstract excerpt
We studied fusion proteins between the human adenosine A1 receptor and different 351Cys-mutated G(i1) alpha-subunits (A1-Gialpha) with respect to two important concepts in receptor pharmacology, i.e. allosteric modulation and constitutive activity/inverse agonism. The aim of our study was twofold. We first analysed whether such fusion products are still subject to allosteric modulation, and, secondly, we...
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