ArticleBritish journal of pharmacology2008
Regulation of two-pore-domain (K2P) potassium leak channels by the tyrosine kinase inhibitor genistein.
Article in British journal of pharmacology, 2008. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 32 papers.
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Who cites it
32 citing papers in PubMed, 67 citations in OpenAlex.
- Article
- KPharmaceuticals (Basel, Switzerland) · 2026Review
- From allergy to arrhythmia - electrophysiological basis for the antiarrhythmic properties of antazoline.Frontiers in pharmacology · 2026Article
- Gating mechanism of the two-pore-domain potassium channel THIK1.Nature structural & molecular biology · 2025Article
- Electrophysiological Effects of the Sodium-Glucose Co-Transporter-2 (SGLT2) Inhibitor Dapagliflozin on Human Cardiac Potassium Channels.International journal of molecular sciences · 2024Article
- The Advantages, Challenges, and Future of Human-Induced Pluripotent Stem Cell Lines in Type 2 Long QT Syndrome.Journal of cardiovascular translational research · 2023Review
- Flavonoids as Modulators of Potassium Channels.International journal of molecular sciences · 2023Review
- KCNK9 mediates the inhibitory effects of genistein on hepatic metastasis from colon cancer.Clinics (Sao Paulo, Brazil) · 2023Article
- Two-Pore-Domain Potassium (KCells · 2021Review
- Bitter taste receptor agonists regulate epithelial two-pore potassium channels via cAMP signaling.Respiratory research · 2021Article
- Article
- N-glycosylation-dependent regulation of hKMolecular biology of the cell · 2019Article
- Antiarrhythmic Properties of Ranolazine: Inhibition of Atrial Fibrillation Associated TASK-1 Potassium Channels.Frontiers in pharmacology · 2019Article
- Cardiovascular pharmacology of KNaunyn-Schmiedeberg's archives of pharmacology · 2018Article
- Physiological genomics identifies genetic modifiers of long QT syndrome type 2 severity.The Journal of clinical investigation · 2018Article
- Acetylcholine-dependent upregulation of TASK-1 channels in thalamic interneurons by a smooth muscle-like signalling pathway.The Journal of physiology · 2017Article
- Effect of tyrphostin AG879 on Kv 4.2 and Kv 4.3 potassium channels.British journal of pharmacology · 2015Article
- Modulation of K2P 2.1 and K2P 10.1 K(+) channel sensitivity to carvedilol by alternative mRNA translation initiation.British journal of pharmacology · 2014Article
- THIK-1 (K2P13.1) is a small-conductance background K(+) channel in rat trigeminal ganglion neurons.Pflugers Archiv : European journal of physiology · 2014Article
- Functional characterization of zebrafish K2P18.1 (TRESK) two-pore-domain K+ channels.Naunyn-Schmiedeberg's archives of pharmacology · 2014Article
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Authors and funding
13 authors at 3 institutions in 2 countries.
Funding
Abstract
background and purposeTwo-pore-domain potassium (K2P) channels mediate potassium background (or 'leak') currents, controlling excitability by stabilizing membrane potential below firing threshold and expediting repolarization. Inhibition of K2P currents permits membrane potential depolarization and excitation. As expected for key regulators of excitability, leak channels are under tight control from a plethora of stimuli. Recently, signalling via protein tyrosine kinases (TKs) has been implicated in ion channel modulation. The objective of this study was to investigate TK regulation of K2P channels. EXPERIMENTAL APPROACH: The two-electrode voltage clamp technique was used to record K2P currents in Xenopus oocytes. In addition, K2P channels were studied in Chinese hamster ovary (CHO) cells using the whole-cell patch clamp technique. KEY
resultsHere, we report inhibition of human K2P3.1 (TASK-1) currents by the TK antagonist, genistein, in Xenopus oocytes (IC50=10.7 microM) and in CHO cells (IC50=12.3 microM). The underlying molecular mechanism was studied in detail. hK2P3.1 was not affected by genistin, an inactive analogue of genistein. Perorthovanadate, an inhibitor of tyrosine phosphatase activity, reduced the inhibitory effect of genistein. Current reduction was voltage independent and did not require channel protonation at position H98 or phosphorylation at the single TK phosphorylation site, Y323. Among functional hK2P family members, genistein also reduced K2P6.1 (TWIK-2), K2P9.1 (TASK-3) and K2P13.1 (THIK-1) currents, respectively. CONCLUSIONS AND IMPLICATIONS: Modulation of K2P channels by the TK inhibitor, genistein, represents a novel molecular mechanism to alter background K+ currents.
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