Antidepressive and anxiolytic effects of ostruthin, a TREK-1 channel activator. [PDF]
PLoS ONE, 2018 We screened a library of botanical compounds purified from plants of Vietnam for modulators of the activity of a two-pore domain K+ channel, TREK-1, and we identified a hydroxycoumarin-related compound, ostruthin, as an activator of this channel ...
Ancy Joseph +3 more
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Aggregation-Induced Emission: Lighting Up hERG Potassium Channel [PDF]
Frontiers in Chemistry, 2019 Based on the scaffold of astemizole and E-4031, four AIE light-up probes (L1–L4) for Human Ether-a-go-go-Related Gene (hERG) potassium channel were developed herein using AIE fluorogen(TPE).
Xiaomeng Zhang +4 more
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Intracellular hemin is a potent inhibitor of the voltage-gated potassium channel Kv10.1 [PDF]
Scientific Reports, 2022 Heme, an iron-protoporphyrin IX complex, is a cofactor bound to various hemoproteins and supports a broad range of functions, such as electron transfer, oxygen transport, signal transduction, and drug metabolism. In recent years, there has been a growing
Nirakar Sahoo +11 more
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Natural antisense transcripts regulate the neuronal stress response and excitability [PDF]
eLife, 2014 Neurons regulate ionic fluxes across their plasma membrane to maintain their excitable properties under varying environmental conditions. However, the mechanisms that regulate ion channels abundance remain poorly understood.
Xingguo Zheng +3 more
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The potassium channel Ether à go-go is a novel prognostic factor with functional relevance in acute myeloid leukemia [PDF]
Molecular Cancer, 2010 AbstractBackgroundThe voltage-gated potassium channel hEag1 (KV10.1) has been related to cancer biology. The physiological expression of the human channel is restricted to the brain but it is frequently and abundantly expressed in many solid tumors, thereby making it a promising target for a specific diagnosis and therapy.
Jasmin R. Agarwal +3 more
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Structural basis of action for a human ether-a-go-go-related gene 1 potassium channel activator [PDF]
Proceedings of the National Academy of Sciences, 2007 Activation of human ether-a-go-go-related gene 1 (hERG1) K + channels mediates cardiac action potential repolarization. Drugs that activate hERG1 channels represent a mechanism-based approach for the treatment of long QT syndrome, a disorder of cardiac repolarization associated with ventricular arrhythmia and sudden
Matthew D. Perry +2 more
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Potassium dependent structural changes in the selectivity filter of HERG potassium channels [PDF]
Nature CommunicationsThe fine tuning of biological electrical signaling is mediated by variations in the rates of opening and closing of gates that control ion flux through different ion channels. Human ether-a-go-go related gene (HERG) potassium channels have uniquely rapid
Carus H. Y. Lau +10 more
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Molecular basis of slow activation of the human ether‐á‐go‐go related gene potassium channel [PDF]
The Journal of Physiology, 2004 The human ether‐á‐go‐go related gene (HERG) encodes the pore forming α‐subunit of the rapid delayed rectifier K+ channel which is central to the repolarization phase of the cardiac action potential. HERG K+ channels have unusual kinetics characterized by slow activation and deactivation, yet rapid inactivation.
Rajesh Subbiah +5 more
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Human ether-à-go-go gene potassium channels are regulated by EGFR tyrosine kinase
Biochimica et Biophysica Acta (BBA) - Molecular Cell Research, 2011 Human ether á-go-go gene potassium channels (hEAG1 or Kv10.1) are expressed in brain and various human cancers and play a role in neuronal excitement and tumor progression. However, the functional regulation of hEAG channels by signal transduction is not fully understood.
Wei Wu +6 more
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Rac and Rho Mediate Opposing Hormonal Regulation of the Ether-A-Go-Go-Related Potassium Channel [PDF]
Current Biology, 2002 Previous studies of ion channel regulation by G proteins have focused on the larger, heterotrimeric GTPases, which are activated by heptahelical membrane receptors. In contrast, studies of the Rho family of smaller, monomeric, Ras-related GTPases, which are activated by cytoplasmic guanine nucleotide exchange factors, have focused on their role in ...
Nina M. Storey +2 more
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