title: Styrax blocks inward and outward current of Kir2.1 channel.
abstract: Kir2.1 plays key roles in setting rest membrane potential and modulation of cell excitability. Mutations of Kir2.1, such as D172N or E299V, inducing gain-of-function, can cause type3 short QT syndrome (SQT3) due to the enlarged outward currents. So far, there is no clinical drug target to block the currents of Kir2.1. Here, we identified a novel blocker of Kir2.1, styrax, which is a kind of natural compound selected from traditional Chinese medicine. Our data show that styrax can abolish the inward and outward currents of Kir2.1. The IC50of styrax for WT, D172N and E299V are 0.0113 ± 0.00075, 0.0204 ± 0.0048 and 0.0122 ± 0.0012 (in volume), respectively. The results indicate that styrax can serve as a novel blocker for Kir2.1.
authors.affiliation: a Key Laboratory of Molecular Biophysics, Hebei Province, Institute of Biophysics, School of Sciences, Hebei University of Technology , Tianjin , China.
authors.forename: Shuxi
authors.initials: S
authors.lastname: Ren
authors.affiliation: a Key Laboratory of Molecular Biophysics, Hebei Province, Institute of Biophysics, School of Sciences, Hebei University of Technology , Tianjin , China.
authors.forename: Chunli
authors.initials: C
authors.lastname: Pang
authors.affiliation: a Key Laboratory of Molecular Biophysics, Hebei Province, Institute of Biophysics, School of Sciences, Hebei University of Technology , Tianjin , China.
authors.forename: Junwei
authors.initials: J
authors.lastname: Li
authors.affiliation: a Key Laboratory of Molecular Biophysics, Hebei Province, Institute of Biophysics, School of Sciences, Hebei University of Technology , Tianjin , China.
authors.forename: Yayue
authors.initials: Y
authors.lastname: Huang
authors.affiliation: a Key Laboratory of Molecular Biophysics, Hebei Province, Institute of Biophysics, School of Sciences, Hebei University of Technology , Tianjin , China.
authors.forename: Suhua
authors.initials: S
authors.lastname: Zhang
authors.affiliation: a Key Laboratory of Molecular Biophysics, Hebei Province, Institute of Biophysics, School of Sciences, Hebei University of Technology , Tianjin , China.
authors.forename: Yong
authors.initials: Y
authors.lastname: Zhan
authors.affiliation: a Key Laboratory of Molecular Biophysics, Hebei Province, Institute of Biophysics, School of Sciences, Hebei University of Technology , Tianjin , China.
authors.forename: Hailong
authors.initials: H
authors.lastname: An
mesh_terms: D057809:HEK293 Cells; D006801:Humans; D008516:Medicine, Chinese Traditional; D028321:Plant Preparations / Q000494:pharmacology*; D026902:Potassium Channel Blockers / Q000494:pharmacology*; D024661:Potassium Channels, Inwardly Rectifying / Q000037:antagonists & inhibitors* / Q000502:physiology; D032362:Styrax
chemical_list: C489461:Kir2.1 channel; D028321:Plant Preparations; D026902:Potassium Channel Blockers; D024661:Potassium Channels, Inwardly Rectifying
keywords: Kir2.1; SQT3; bloker; fluxOR™; ion channel; patch clamp; styrax