Disulphide trapping of the GABA(A) receptor reveals the importance of the coupling interface in the action of benzodiazepines.

@article{Hanson2011DisulphideTO,
  title={Disulphide trapping of the GABA(A) receptor reveals the importance of the coupling interface in the action of benzodiazepines.},
  author={Susan M. Hanson and Cynthia Czajkowski},
  journal={British journal of pharmacology},
  year={2011},
  volume={162 3},
  pages={673-87}
}
BACKGROUND AND SIGNIFICANCE Although the functional effects of benzodiazepines (BZDs) on GABA(A) receptors have been well characterized, the structural mechanism by which these modulators alter activation of the receptor by GABA is still undefined. EXPERIMENTAL APPROACH We used disulphide trapping between engineered cysteines to probe BZD-induced conformational changes within the γ₂ subunit and at the α₁/γ₂ coupling interface (Loops 2, 7 and 9) of α₁β₂γ₂ GABA(A) receptors. KEY RESULTS… CONTINUE READING
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