Nature Communications (Oct 2016)
KCNE1 induces fenestration in the Kv7.1/KCNE1 channel complex that allows for highly specific pharmacological targeting
- Eva Wrobel,
- Ina Rothenberg,
- Christoph Krisp,
- Franziska Hundt,
- Benjamin Fraenzel,
- Karina Eckey,
- Joannes T. M. Linders,
- David J. Gallacher,
- Rob Towart,
- Lutz Pott,
- Michael Pusch,
- Tao Yang,
- Dan M. Roden,
- Harley T. Kurata,
- Eric Schulze-Bahr,
- Nathalie Strutz-Seebohm,
- Dirk Wolters,
- Guiscard Seebohm
Affiliations
- Eva Wrobel
- Department of Cardiovascular Medicine, Institute for Genetics of Heart Diseases (IfGH), University Hospital Muenster
- Ina Rothenberg
- Department of Cardiovascular Medicine, Institute for Genetics of Heart Diseases (IfGH), University Hospital Muenster
- Christoph Krisp
- Department of Analytical Chemistry, Ruhr University of Bochum
- Franziska Hundt
- Department of Analytical Chemistry, Ruhr University of Bochum
- Benjamin Fraenzel
- Department of Analytical Chemistry, Ruhr University of Bochum
- Karina Eckey
- Department of Cardiovascular Medicine, Institute for Genetics of Heart Diseases (IfGH), University Hospital Muenster
- Joannes T. M. Linders
- a Division of Janssen Pharmaceutica N.V., Project Management Office, Janssen Research & Development
- David J. Gallacher
- a Division of Janssen Pharmaceutica N.V., Safety Pharmacology Research, Translational Sciences, Janssen Research & Development
- Rob Towart
- a Division of Janssen Pharmaceutica N.V., Safety Pharmacology Research, Translational Sciences, Janssen Research & Development
- Lutz Pott
- Institute of Physiology, Ruhr University of Bochum
- Michael Pusch
- Istituto di Biofisica CNR
- Tao Yang
- Departments of Medicine, Vanderbilt University School of Medicine
- Dan M. Roden
- Departments of Medicine, Pharmacology and Biomedical Informatics, Vanderbilt University School of Medicine
- Harley T. Kurata
- Department of Pharmacology, University of Alberta
- Eric Schulze-Bahr
- Department of Cardiovascular Medicine, Institute for Genetics of Heart Diseases (IfGH), University Hospital Muenster
- Nathalie Strutz-Seebohm
- Department of Cardiovascular Medicine, Institute for Genetics of Heart Diseases (IfGH), University Hospital Muenster
- Dirk Wolters
- Department of Analytical Chemistry, Ruhr University of Bochum
- Guiscard Seebohm
- Department of Cardiovascular Medicine, Institute for Genetics of Heart Diseases (IfGH), University Hospital Muenster
- DOI
- https://doi.org/10.1038/ncomms12795
- Journal volume & issue
-
Vol. 7,
no. 1
pp. 1 – 13
Abstract
Specificity of inhibitors of voltage-gated ion channels is crucial for their use as therapeutics. Here, the authors show that adamantane derivatives interact with a specific binding site on fenestrations that only become available when accessory subunits are bound to the channel.