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题目:: Impact of fusion to Gα(i2) and co-expression with RGS proteins on pharmacological properties of human cannabinoid receptors CB₁R and CB₂R.
作者:: Sutor(Sarah),Heilmann(Jörg),Seifert(Roland)
状态:: 发布时间2011-07-01 , 更新时间 2011-07-01
期刊:: J Pharm Pharmacol
摘要:: G protein coupled receptor (GPCR)-Gα fusion proteins are often employed to investigate receptor/G protein interaction. In this study, the impact of Gα fusion proteins on pharmacology of CBRs, both mediating signals through Gα(i) proteins, were investigated. Gα(i2) was fused to the C-terminus of the CBRs or co-expressed with non-fused Gα(i2) in Sf9 cells, always together with Gβ₁γ₂. Furthermore, the impact of RGS proteins on CBR signaling in combination with the CBR fusion approach was examined, using RGS4 and RGS19 as paradigms.,CBR ligands were characterized in the steady-state GTPase assay and pharmacological properties of ligands in the different test systems were correlated.,Fusion of CBRs to Gα(i2) enhanced the maximal stimulatory effects of ligands compared to the co-expression system, especially for CB₂R. RGS4, but not RGS19, behaved as a GTPase-activating protein at CBRs in the Gα(i2) co-expression and fusion system. Fusion of GPCR, most prominently CB₂R, to Gα(i2) , and co-expression with RGS4 altered the pharmacological properties of ligands.,Our data suggest that fusion of CB₂R to Gα(i2) and co-expression with RGS4 impedes with conformational changes. Moreover, our results support the concept of ligand-specific receptor conformations. Finally, this paper describes the most sensitive CBR test system currently available.
语言:: eng
DOI:: 10.1111/j.2042-7158.2011.01307.x

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