Journal ArticleDOI
Potassium Channels: Structures, Diseases, and Modulators
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TLDR
This review tries to summarize the latest developments in structure determinants and regulation mechanism of all types of potassium channels and proves that modulators possess some certain natural‐product scaffolds and pharmacokinetic parameters are important properties for organic molecules.Abstract:
Potassium channels participate in many critical biological functions and play important roles in a variety of diseases. In recent years, many significant discoveries have been made which motivate us to review these achievements. The focus of our review is mainly on three aspects. Firstly, we try to summarize the latest developments in structure determinants and regulation mechanism of all types of potassium channels. Secondly, we review some diseases induced by or related to these channels. Thirdly, both qualitative and quantitative approaches are utilized to analyze structural features of modulators of potassium channels. Our analyses further prove that modulators possess some certain natural-product scaffolds. And pharmacokinetic parameters are important properties for organic molecules. Besides, with in silico methods, some features that can be used to differentiate modulators are derived. There is no doubt that all these studies on potassium channels as possible pharmaceutical targets will facilitate future translational research. All the strategies developed in this review could be extended to studies on other ion channels and proteins as well.read more
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Molecular mechanisms of action of systemic lidocaine in acute and chronic pain: a narrative review
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Novel genetically encoded fluorescent probes enable real-time detection of potassium in vitro and in vivo.
Helmut Bischof,Markus Rehberg,Sarah Stryeck,Katharina Artinger,Emrah Eroglu,Markus Waldeck-Weiermair,Benjamin Gottschalk,Rene Rost,Andras T. Deak,Tobias Niedrist,Nemanja Vujic,Hanna Lindermuth,Ruth Prassl,Brigitte Pelzmann,Klaus Groschner,Dagmar Kratky,Kathrin Eller,Alexander R. Rosenkranz,Tobias Madl,Nikolaus Plesnila,Wolfgang F. Graier,Roland Malli +21 more
TL;DR: K+ plays an important role in physiology and disease, but the lack of high specificity K+ sensors limits the understanding of its spatiotemporal dynamics, so genetically-encoded FRET-based probes able to quantify K+ concentration in body fluids, cells and specific organelles are developed.
Journal ArticleDOI
Mutations in the voltage-gated potassium channel gene KCNH1 cause Temple-Baraitser syndrome and epilepsy
Cas Simons,Lachlan D. Rash,Joanna Crawford,Linlin Ma,Ben Cristofori-Armstrong,David Miller,Kelin Ru,Gregory J. Baillie,Yasemin Alanay,Adeline Jacquinet,François-Guillaume Debray,Alain Verloes,Joseph J. Shen,Gozde Yesil,Serhat Guler,Adnan Yuksel,John G. Cleary,Sean M. Grimmond,Julie McGaughran,Glenn F. King,Michael T. Gabbett,Ryan J. Taft +21 more
TL;DR: Damaging de novo mutations in KCNH1, a voltage-gated potassium channel that is predominantly expressed in the central nervous system (CNS), are reported in six individuals with Temple-Baraitser syndrome, demonstrating that the etiology of many unresolved CNS disorders, including epilepsies, might be explained by pathogenic mosaic mutations.
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Effects of monoterpenes on ion channels of excitable cells
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References
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Journal ArticleDOI
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Declan A. Doyle,João H.Morais Cabral,Richard A. Pfuetzner,Anling Kuo,Jacqueline M. Gulbis,Steven L. Cohen,Brian T. Chait,Roderick MacKinnon +7 more
TL;DR: The architecture of the pore establishes the physical principles underlying selective K+ conduction, which promotes ion conduction by exploiting electrostatic repulsive forces to overcome attractive forces between K+ ions and the selectivity filter.
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Journal ArticleDOI
A mechanistic link between an inherited and an acquird cardiac arrthytmia: HERG encodes the IKr potassium channel
TL;DR: The finding that HERG encodes IKr channels provides a mechanistic link between certain forms of inherited and acquired LQT, and that an additional subunit may be required for drug sensitivity.
Journal ArticleDOI
A molecular basis for cardiac arrhythmia: HERG mutations cause long QT syndrome
Mark E. Curran,Igor Splawski,Katherine W. Timothy,Vincent Gm,Eric D. Green,Keating Mt,Keating Mt +6 more
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