Photo-antagonism of the GABAA receptor

Martin Mortensen, Favaad Iqbal, Arun P. Pandurangan, Saad Hannan, Rosemary Huckvale, Maya Topf, James R. Baker and Trevor G. Smart ()
Additional contact information
Martin Mortensen: Physiology and Pharmacology, University College London
Favaad Iqbal: University College London
Arun P. Pandurangan: Institute of Structural and Molecular Biology, Birkbeck College, University of London
Saad Hannan: Physiology and Pharmacology, University College London
Rosemary Huckvale: University College London
Maya Topf: Institute of Structural and Molecular Biology, Birkbeck College, University of London
James R. Baker: University College London
Trevor G. Smart: Physiology and Pharmacology, University College London

Nature Communications, 2014, vol. 5, issue 1, 1-13

Abstract: Abstract Neurotransmitter receptor trafficking is fundamentally important for synaptic transmission and neural network activity. GABAA receptors and inhibitory synapses are vital components of brain function, yet much of our knowledge regarding receptor mobility and function at inhibitory synapses is derived indirectly from using recombinant receptors, antibody-tagged native receptors and pharmacological treatments. Here we describe the use of a set of research tools that can irreversibly bind to and affect the function of recombinant and neuronal GABAA receptors following ultraviolet photoactivation. These compounds are based on the competitive antagonist gabazine and incorporate a variety of photoactive groups. By using site-directed mutagenesis and ligand-docking studies, they reveal new areas of the GABA binding site at the interface between receptor β and α subunits. These compounds enable the selected inactivation of native GABAA receptor populations providing new insight into the function of inhibitory synapses and extrasynaptic receptors in controlling neuronal excitation.

Date: 2014
References: Add references at CitEc
Citations:

Downloads: (external link)
https://www.nature.com/articles/ncomms5454 Abstract (text/html)

Related works:
This item may be available elsewhere in EconPapers: Search for items with the same title.

Export reference: BibTeX RIS (EndNote, ProCite, RefMan) HTML/Text

Persistent link: https://EconPapers.repec.org/RePEc:nat:natcom:v:5:y:2014:i:1:d:10.1038_ncomms5454

Ordering information: This journal article can be ordered from
https://www.nature.com/ncomms/

DOI: 10.1038/ncomms5454

Access Statistics for this article

Nature Communications is currently edited by Nathalie Le Bot, Enda Bergin and Fiona Gillespie

More articles in Nature Communications from Nature
Bibliographic data for series maintained by Sonal Shukla () and Springer Nature Abstracting and Indexing ().