The role of transcriptional and translational mechanisms in flumazenil-induced up-regulation of recombinant GABAA receptors

@article{Jembrek2008TheRO,
  title={The role of transcriptional and translational mechanisms in flumazenil-induced up-regulation of recombinant GABAA receptors},
  author={Maja Jazvin{\vs}{\'c}ak Jembrek and Dubravka {\vS}vob {\vS}trac and Josipa Vlaini{\'c} and Danka Peri{\vc}i{\'c}},
  journal={Neuroscience Research},
  year={2008},
  volume={61},
  pages={234-241}
}
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References

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Chronic flumazenil alters GABA(A) receptor subunit mRNA expression, translation product assembly and channel function in neuronal cultures.
TLDR
Double-immunolabeling experiments using 5- and 10-nm gold particles suggest that after chronic flumazenil treatment, receptor subunit assemblies containing the alpha1/gamma2 and alpha6/delta subunits may be replaced by a receptor assembly containing thealpha1/d delta subunits.
Benzodiazepine Treatment Causes Uncoupling of Recombinant GABAA Receptors Expressed in Stably Transfected Cells
TLDR
The uncoupling observed in this system was not accompanied by receptor internalization, is unlikely to be due to changes in receptor subunit composition, and probably represents posttranslational changes, and the rapid regulation of allosteric coupling by benzodiazepine treatment of the stably transfected cells should provide insights to the mechanisms of coupling between GABAA and benzodiazine receptors as well as benzODiazepine tolerance.
Mechanisms of up-regulation of D2L dopamine receptors by agonists and antagonists in transfected HEK-293 cells.
TLDR
Results of experiments with cycloheximide, a protein-synthesis inhibitor, suggest that increased protein synthesis, and not decreased protein degradation, is responsible for up-regulation by both NPA and (-)-sulpiride.
Chronic benzodiazepine treatment of cells expressing recombinant GABAA receptors uncouples allosteric binding: studies on possible mechanisms
TLDR
Mutation of the only PKAosphorylation site expressed from among the subunits proved that direct phosphorylation of the GABAR was not involved in either coupling after chronic BZ exposure or reversal of uncoupling after exposure to the competitive BZ antagonist, flumazenil.
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