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Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)
 

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Gene Review: 

GABA-B-R2  -  metabotropic GABA-B receptor subtype 2

Drosophila melanogaster

Synonyms: BcDNA:GH07312, CG6706, D-GABA[[B]]R2, D-Gaba2, Dmel\CG6706, ...
 
 
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High impact information on GABA-B-R2

  • Our data show that mutations of specific amino acids in GB2 can induce agonism in addition to positive modulation and facilitate GB2 activation in the absence of GB1 [1].
  • GS39783 positively modulated GABA responses but also showed considerable agonistic activity at heterodimers containing a mutant rat GB2 subunit with three amino acid substitutions in transmembrane domain VI [1].
  • So far, there has been no direct demonstration that GB2 binds GABA or another endogenous ligand [2].
  • This suggests that the GB2 VFTM does not constitute a binding site for a natural ligand [2].
  • Finally, although in either GB1 or the related metabotropic glutamate receptors most residues of the binding pocket are conserved from Caenorhabditis elegans to human, no such conservation is observed in GB2 [2].
 

Other interactions of GABA-B-R2

  • Moreover, GB2 is required for the high agonist affinity of GB1 [2].

References

  1. Point Mutations in the Transmembrane Region of GABAB2 Facilitate Activation by the Positive Modulator N,N'-Dicyclopentyl-2-methylsulfanyl-5-nitro-pyrimidine-4,6-diamine (GS39783) in the Absence of the GABAB1 Subunit. Dupuis, D.S., Relkovic, D., Lhuillier, L., Mosbacher, J., Kaupmann, K. Mol. Pharmacol. (2006) [Pubmed]
  2. No ligand binding in the GB2 subunit of the GABA(B) receptor is required for activation and allosteric interaction between the subunits. Kniazeff, J., Galvez, T., Labesse, G., Pin, J.P. J. Neurosci. (2002) [Pubmed]
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