Analysis of Differential Efficacy and Affinity of GABAA (α1/α2) Selective Modulators.

@article{Ain2016AnalysisOD,
  title={Analysis of Differential Efficacy and Affinity of GABAA ($\alpha$1/$\alpha$2) Selective Modulators.},
  author={Q. Ain and R. M. Owen and K. Omoto and Rubben Torella and Krishna C. Bulusu and D. Pryde and R. Glen and Julian E. Fuchs and A. Bender},
  journal={Molecular pharmaceutics},
  year={2016},
  volume={13 11},
  pages={
          4001-4012
        }
}
Selective modulators of the γ-amino butyric acid (GABAA) family of receptors have the potential to treat a range of disease states related to cognition, pain, and anxiety. While the development of various α subunit-selective modulators is currently underway for the treatment of anxiety disorders, a mechanistic understanding of the correlation between their bioactivity and efficacy, based on ligand-target interactions, is currently still lacking. In order to alleviate this situation, in the… Expand
Cross-talk between allosteric and orthosteric binding sites of γ-amino butyric acid type A receptors (GABAA-Rs): A computational study revealing the structural basis of selectivity
TLDR
Early stages of allosteric modulation are revealed, highlighting subtype selective activation and pathways recommending GABA binding sites during selective modulation, to enable better α2-selective modulator/s. Expand

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