KCNE1 induces fenestration in the Kv7.1/KCNE1 channel complex that allows for highly specific pharmacological targeting
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.
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| Format: | Article |
| Language: | English |
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Nature Publishing Group
2016-10-01
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| Series: | Nature Communications |
| Online Access: | https://doi.org/10.1038/ncomms12795 |
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doaj-6f13dc5b883d4828afc6c8522bd13d5d2021-05-11T10:44:39ZengNature Publishing GroupNature Communications2041-17232016-10-017111310.1038/ncomms12795KCNE1 induces fenestration in the Kv7.1/KCNE1 channel complex that allows for highly specific pharmacological targetingEva Wrobel0Ina Rothenberg1Christoph Krisp2Franziska Hundt3Benjamin Fraenzel4Karina Eckey5Joannes T. M. Linders6David J. Gallacher7Rob Towart8Lutz Pott9Michael Pusch10Tao Yang11Dan M. Roden12Harley T. Kurata13Eric Schulze-Bahr14Nathalie Strutz-Seebohm15Dirk Wolters16Guiscard Seebohm17Department of Cardiovascular Medicine, Institute for Genetics of Heart Diseases (IfGH), University Hospital MuensterDepartment of Cardiovascular Medicine, Institute for Genetics of Heart Diseases (IfGH), University Hospital MuensterDepartment of Analytical Chemistry, Ruhr University of BochumDepartment of Analytical Chemistry, Ruhr University of BochumDepartment of Analytical Chemistry, Ruhr University of BochumDepartment of Cardiovascular Medicine, Institute for Genetics of Heart Diseases (IfGH), University Hospital Muenstera Division of Janssen Pharmaceutica N.V., Project Management Office, Janssen Research & Developmenta Division of Janssen Pharmaceutica N.V., Safety Pharmacology Research, Translational Sciences, Janssen Research & Developmenta Division of Janssen Pharmaceutica N.V., Safety Pharmacology Research, Translational Sciences, Janssen Research & DevelopmentInstitute of Physiology, Ruhr University of BochumIstituto di Biofisica CNRDepartments of Medicine, Vanderbilt University School of MedicineDepartments of Medicine, Pharmacology and Biomedical Informatics, Vanderbilt University School of MedicineDepartment of Pharmacology, University of AlbertaDepartment of Cardiovascular Medicine, Institute for Genetics of Heart Diseases (IfGH), University Hospital MuensterDepartment of Cardiovascular Medicine, Institute for Genetics of Heart Diseases (IfGH), University Hospital MuensterDepartment of Analytical Chemistry, Ruhr University of BochumDepartment of Cardiovascular Medicine, Institute for Genetics of Heart Diseases (IfGH), University Hospital MuensterSpecificity 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.https://doi.org/10.1038/ncomms12795 |
| collection |
DOAJ |
| language |
English |
| format |
Article |
| sources |
DOAJ |
| author |
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 |
| spellingShingle |
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 KCNE1 induces fenestration in the Kv7.1/KCNE1 channel complex that allows for highly specific pharmacological targeting Nature Communications |
| author_facet |
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 |
| author_sort |
Eva Wrobel |
| title |
KCNE1 induces fenestration in the Kv7.1/KCNE1 channel complex that allows for highly specific pharmacological targeting |
| title_short |
KCNE1 induces fenestration in the Kv7.1/KCNE1 channel complex that allows for highly specific pharmacological targeting |
| title_full |
KCNE1 induces fenestration in the Kv7.1/KCNE1 channel complex that allows for highly specific pharmacological targeting |
| title_fullStr |
KCNE1 induces fenestration in the Kv7.1/KCNE1 channel complex that allows for highly specific pharmacological targeting |
| title_full_unstemmed |
KCNE1 induces fenestration in the Kv7.1/KCNE1 channel complex that allows for highly specific pharmacological targeting |
| title_sort |
kcne1 induces fenestration in the kv7.1/kcne1 channel complex that allows for highly specific pharmacological targeting |
| publisher |
Nature Publishing Group |
| series |
Nature Communications |
| issn |
2041-1723 |
| publishDate |
2016-10-01 |
| description |
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. |
| url |
https://doi.org/10.1038/ncomms12795 |
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