Inhibition of human ether a go-go potassium channels by Ca2+/calmodulin [PDF]
Intracellular Ca(2+) inhibits voltage-gated potassium channels of the ether à go-go (EAG) family. To identify the underlying molecular mechanism, we expressed the human version hEAG1 in Xenopus oocytes. The channels lost Ca(2+) sensitivity when measured in cell-free membrane patches.
Roland Schönherr
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Ether à go-go potassium channel expression in soft tissue sarcoma patients [PDF]
Abstract Background The expression of the human Eag1 potassium channel (Kv10.1) is normally restricted to the adult brain, but it has been detected in both tumour cell lines and primary tumours. Our purpose was to determine the frequency of expression of Eag1 in soft tissue sarcoma and its potential clinical ...
Fernanda Mello de Queiroz+3 more
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Carboxy-terminal domain mediates assembly of the voltage-gated rat ether-a-go-go potassium channel [PDF]
The specific assembly of subunits to oligomers is an important prerequisite for producing functional potassium channels. We have studied the assembly of voltage-gated rat ether-à-go-go (r-eag) potassium channels with two complementary assays. In protein overlay binding experiments it was shown that a 41-amino-acid domain, close to the r-eag subunit ...
Jost Ludwig
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Activation of human ether-a-go-go related gene (hERG) potassium channels by small molecules [PDF]
Human ether-a-go-go related gene (hERG) potassium (K(+)) channels play a critical role in cardiac action potential repolarization. Mutations that reduce hERG conductance or surface expression may cause congenital long QT syndrome (LQTS). However, the channels can be inhibited by structurally diverse small molecules, resulting in an acquired form of ...
Pingzheng Zhou+4 more
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p38 MAPK regulates the expression of ether à go-go potassium channel in human osteosarcoma cells [PDF]
Abstract Background. The ether à go-go (Eag) channel has been shown to be overexpressed in a variety of cancers. However, the expression and function of Eag in osteosarcoma are poorly understood. In addition, the molecular mechanisms responsible for Eag overexpression in cancer cells remain unclear. Methods.
Xinyu Wu+5 more
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β-Arrestin-Mediated Regulation of the HumanEther-a-go-go-Related Gene Potassium Channel [PDF]
The rapidly activating delayed rectifier K+ channel (IKr) is encoded by the human ether-a-go-go-related gene (hERG), which is important for the repolarization of the cardiac action potential. Mutations in hERG or drugs can impair the function or decrease the expression level of hERG channels, leading to long QT syndrome.
Matthew Sangoi+7 more
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Fluorogenic Probe for the Human Ether-a-Go-Go-Related Gene Potassium Channel Imaging [PDF]
The first small-molecule fluorogenic probe A1 for imaging the human Ether-a-go-go-Related Gene (hERG) potassium channel based on the photoinduced electron transfer (PET) off-on mechanism was described herein. After careful biological evaluation, this probe had the potential of detecting and imaging the hERG channel at the molecular and cellular level ...
Zhenzhen Liu+5 more
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Overexpression of potassium channel ether à go-go in human osteosarcoma
Human ether à go-go (hEAG) potassium channels are primarily expressed in brain but also frequently overexpressed in solid tumors, which could indicate their potential value for cancer diagnosis and therapy. hEAG1, one member of the hEAG subfamily, has been shown to play a role in neoplastic process.
Jingna Wu+5 more
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Comparative effects of azimilide and ambasilide on the human ether-a-go-go-related gene (HERG) potassium channel [PDF]
To evaluate the effects of azimilide and ambasilide on the biophysical properties of the human-ether-a-go-go-related (HERG) channel.HERG was stably transfected into Chinese hamster ovary (CHO-K1) cells and currents were measured using a whole cell, voltage-clamp technique.Azimilide had a 'dual effect', inhibiting current at voltage steps above -40 mV ...
Bruce D. Walker
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Emerging roles for ether‐á‐go‐go‐related gene potassium channels in the brain
Voltage-activated ether-a-go-go-related gene (ERG1a, Kv11) potassium channels play a prominent role in regulating cardiac excitability and in heart disease. Recently, ERG channels were found to be widely distributed in brain (Papa et al. 2003; Guasti et al. 2005), although little is currently known regarding their functional role in the nervous system.
Paul D. Shepard, Matthew C. Trudeau
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