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000839912 020__ $$a0-8412-3258-X (electronic)
000839912 0247_ $$2doi$$a10.1021/bk-2017-1265.ch005
000839912 0247_ $$2ISSN$$a0097-6156
000839912 0247_ $$2ISSN$$a1947-5918
000839912 037__ $$aFZJ-2017-07490
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000839912 1001_ $$0P:(DE-HGF)0$$aGross, Aaron D.$$b0$$eEditor
000839912 245__ $$aSubunit-Specific Modulatory Functions Are Conserved in an Interspecies Insect GABA               B               Receptor Heteromer
000839912 260__ $$aWashington, DC$$bAmerican Chemical Society$$c2017
000839912 29510 $$aAdvances in Agrochemicals: Ion Channels and G Protein-Coupled Receptors (GPCRs) as Targets for Pest Control / Gross, Aaron D. (Editor)   ; Washington, DC : American Chemical Society, 2017,  ; ISSN: 0097-6156=1947-5918 ; ISBN: 0-8412-3260-1=0-8412-3258-X ; doi:10.1021/bk-2017-1265
000839912 300__ $$a85 - 107
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000839912 4900_ $$aACS Symposium Series$$v1265
000839912 520__ $$aGABAB receptors are seven-transmembrane G-protein-coupled receptors (GPCRs) for γ-aminobutyric acid (GABA), the most abundant inhibitory neurotransmitter in the central nervous system. They couple to a variety of signalling pathways and thereby serve diverse functions. In humans, GABAB receptors are implicated in a number of psychiatriac and neurological diseases. GABAB receptors function as obligate heteromers consisting of the two subunits, GB1 and GB2, whereby GB1 binds the ligand and GB2 is coupled to the G protein. This unique functional principle is phylogenetically conserved and can be found in both deuterostomes and protostomes. Nevertheless, remarkable differences in the pharmacological properties do exist between species. In this study, we aimed to investigate the functionality and the pharmacological profile of an interspecies GABAB receptor heteromer, consisting of the GB1 subunit from the American cockroach Periplaneta americana and the GB2 subunit of the fruit fly Drosophila melanogaster. Co-expression of both proteins in a heterologous expression system indeed lead to the formation of functional receptor heteromers. Activation of interspecies heterodimers caused a dose-dependent decrease in the production of cAMP. Moreover, we demonstrate that GB2 modulates not only the potency but also the efficacy of ligand binding.
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000839912 7001_ $$0P:(DE-HGF)0$$aOzoe, Yoshihisa$$b1$$eEditor
000839912 7001_ $$0P:(DE-HGF)0$$aCoats, Joel R.$$b2$$eEditor
000839912 7001_ $$0P:(DE-HGF)0$$aBlankenburg, S.$$b3
000839912 7001_ $$0P:(DE-Juel1)131909$$aBalfanz, S.$$b4$$ufzj
000839912 7001_ $$0P:(DE-Juel1)131911$$aBaumann, A.$$b5$$ufzj
000839912 7001_ $$0P:(DE-HGF)0$$aBlenau, W.$$b6$$eCorresponding author
000839912 773__ $$a10.1021/bk-2017-1265.ch005
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000839912 9141_ $$y2017
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