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Publication : Chemical and genetic engineering of selective ion channel-ligand interactions.

First Author  Magnus CJ Year  2011
Journal  Science Volume  333
Issue  6047 Pages  1292-6
PubMed ID  21885782 Mgi Jnum  J:176207
Mgi Id  MGI:5289713 Doi  10.1126/science.1206606
Citation  Magnus CJ, et al. (2011) Chemical and genetic engineering of selective ion channel-ligand interactions. Science 333(6047):1292-6
abstractText  Ionic flux mediates essential physiological and behavioral functions in defined cell populations. Cell type-specific activators of diverse ionic conductances are needed for probing these effects. We combined chemistry and protein engineering to enable the systematic creation of a toolbox of ligand-gated ion channels (LGICs) with orthogonal pharmacologic selectivity and divergent functional properties. The LGICs and their small-molecule effectors were able to activate a range of ionic conductances in genetically specified cell types. LGICs constructed for neuronal perturbation could be used to selectively manipulate neuron activity in mammalian brains in vivo. The diversity of ion channel tools accessible from this approach will be useful for examining the relationship between neuronal activity and animal behavior, as well as for cell biological and physiological applications requiring chemical control of ion conductance.
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