Journal article

KCTD12 modulation of GABA(B) receptor function

Melody Li, Carol J Milligan, Haiyan Wang, Andrew Walker, Leonid Churilov, Andrew J Lawrence, Christopher A Reid, Seth C Hopkins, Steven Petrou

PHARMACOLOGY RESEARCH & PERSPECTIVES | JOHN WILEY & SONS LTD | Published : 2017

Abstract

The molecular composition and functional diversity of native GABAB receptors (GABABR) are still poorly understood, thus hindering development of selective GABABR ligands. Potassium channel tetramerization domain-containing protein (KCTD) 12 is a GABABR auxiliary subunit and mouse KCTD12 can alter GABABR function. In this study, we sought to characterize the effects of human KCTD12 on GABABR kinetics and pharmacology, using an automated electrophysiological assay. Seizure susceptibility and ethanol consumption were also investigated in a KCTD12 knockout mouse model. Human KCTD12 co-expression altered the kinetics of GABABR-mediated GIRK channels, speeding rates of both activation and desensit..

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Grants

Funding Acknowledgements

This work was supported by the National Health and Medical Research Council (NHMRC, Australia) of which SP and AJL are Fellows. We acknowledge the Victorian Government's Operational Infrastructure Support Program.