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| Home > Publications database > Subunit-Specific Modulatory Functions Are Conserved in an Interspecies Insect GABA B Receptor Heteromer |
| Home > Publications database > Subunit-Specific Modulatory Functions Are Conserved in an Interspecies Insect GABA B Receptor Heteromer |
| Contribution to a book | FZJ-2017-07490 |
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2017
American Chemical Society
Washington, DC
ISBN: 0-8412-3260-1 (print), 0-8412-3258-X (electronic)
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Please use a persistent id in citations: doi:10.1021/bk-2017-1265.ch005
Abstract: GABAB 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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