Inhibition of the ethanol-induced potentiation of α1 glycine receptor by a small peptide that interferes with Gβγ binding.

ABSTRACT:

Background

Gβγ interaction with GlyR is an important determinant in ethanol potentiation of this channel.

Results

A small peptide, RQH(C7), can inhibit ethanol potentiation of GlyR currents.

Conclusion

Results with RQH(C7) indicate that ethanol mediated potentiation of GlyR is in part by Gβγ activation.

Significance

Molecular interaction between Gβγ and GlyR could be used as a target for pharmacological modification of ethanol effects. Previous studies indicate that ethanol can modulate glycine receptors (GlyR), in part, through Gβγ interaction with basic residues in the intracellular loop. In this study, we show that a seven-amino acid peptide (RQH(C7)), which has the primary structure of a motif in the large intracellular loop of GlyR (GlyR-IL), was able to i

SUBMITTER: San Martin L 

PROVIDER: S-EPMC3504784 | biostudies-literature | 2012 Nov

REPOSITORIES: biostudies-literature