dc.contributor.author | An, Dongchen | |
dc.contributor.author | Pinheiro-Junior, Ernesto Lopes | |
dc.contributor.author | Béress, László | |
dc.contributor.author | Gladkikh, Irina | |
dc.contributor.author | Leychenko, Elena | |
dc.contributor.author | Undheim, Eivind Andreas Baste | |
dc.contributor.author | Peigneur, Steve | |
dc.contributor.author | Tytgat, Jan | |
dc.date.accessioned | 2023-01-31T15:41:31Z | |
dc.date.available | 2023-01-31T15:41:31Z | |
dc.date.created | 2022-04-29T12:53:20Z | |
dc.date.issued | 2022 | |
dc.identifier.citation | Marine Drugs. 2022, 20 (2), . | en_US |
dc.identifier.issn | 1660-3397 | |
dc.identifier.uri | https://hdl.handle.net/11250/3047501 | |
dc.description.abstract | (1) Background: G protein-coupled inward-rectifier potassium (GIRK) channels, especially neuronal GIRK1/2 channels, have been the focus of intense research interest for developing drugs against brain diseases. In this context, venom peptides that selectively activate GIRK channels can be seen as a new source for drug development. Here, we report on the identification and electrophysiological characterization of a novel activator of GIRK1/2 channels, AsKC11, found in the venom of the sea anemone Anemonia sulcata. (2) Methods: AsKC11 was purified from the sea anemone venom by reverse-phase chromatography and the sequence was identified by mass spectrometry. Using the two-electrode voltage-clamp technique, the activity of AsKC11 on GIRK1/2 channels was studied and its selectivity for other potassium channels was investigated. (3) Results: AsKC11, a Kunitz peptide found in the venom of A. sulcata, is the first peptide shown to directly activate neuronal GIRK1/2 channels independent from Gi/o protein activity, without affecting the inward-rectifier potassium channel (IRK1) and with only a minor effect on KV1.6 channels. Thus, AsKC11 is a novel activator of GIRK channels resulting in larger K+ currents because of an increased chord conductance. (4) Conclusions: These discoveries provide new insights into a novel class of GIRK activators. | en_US |
dc.language.iso | eng | en_US |
dc.publisher | MDPI | en_US |
dc.rights | Navngivelse 4.0 Internasjonal | * |
dc.rights.uri | http://creativecommons.org/licenses/by/4.0/deed.no | * |
dc.title | AsKC11, a Kunitz Peptide from Anemonia sulcata, Is a Novel Activator of G Protein-Coupled Inward-Rectifier Potassium Channels | en_US |
dc.title.alternative | AsKC11, a Kunitz Peptide from Anemonia sulcata, Is a Novel Activator of G Protein-Coupled Inward-Rectifier Potassium Channels | en_US |
dc.type | Peer reviewed | en_US |
dc.type | Journal article | en_US |
dc.description.version | publishedVersion | en_US |
dc.source.pagenumber | 15 | en_US |
dc.source.volume | 20 | en_US |
dc.source.journal | Marine Drugs | en_US |
dc.source.issue | 2 | en_US |
dc.identifier.doi | 10.3390/md20020140 | |
dc.identifier.cristin | 2020126 | |
cristin.ispublished | true | |
cristin.fulltext | original | |
cristin.qualitycode | 1 | |