NBD-Based Environment-Sensitive Fluorescent Probes for the Human Ether-a-Go-Go–Related Gene Potassium Channel [PDF]
Three environment-sensitive probes were developed for the hERG channel based on the nitrobenzoxadiazole fluorophore herein. After careful evaluation, probes M1 and M3 were found to have a high affinity for imaging the hERG channel in the cell-based experiment.
Qi Li +4 more
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Ether-a-go-go Related Gene Potassium Channels: What's All the Buzz About? [PDF]
Antipsychotic drugs are thought to exert their therapeutic action by antagonizing dopamine receptors but are also known to produce side effects in the heart by inhibiting cardiac ether-a-go-go-related gene (ERG) K(+) channels. Recently, it has been discovered that the same channels are present in the brain, including midbrain dopamine neurons.
Donald S. Shepard +2 more
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Non-cancer to anti-cancer: investigation of human ether-a-go-go-related gene potassium channel inhibitors as potential therapeutics [PDF]
Abstract Background The expression of hERG K+ channels is observed in various cancer cells including epithelial, neuronal, leukemic, and connective tissue. The role of hERG potassium channels in regulating the growth and death of cancer cells include cell proliferation, survival, secretion of proangiogenic factors ...
Vaishali M. Patil +3 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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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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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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Blockade of the Human Ether A-Go-Go–Related Gene (hERG) Potassium Channel by Fentanyl [PDF]
The human ether-a-go-go-related gene (hERG) encodes the pore-forming subunit of the rapidly activating delayed rectifier potassium channel (IKr). Drug-mediated or medical condition-mediated disruption of hERG function is the primary cause of acquired long-QT syndrome, which predisposes affected individuals to ventricular arrhythmias and sudden death ...
Jared Tschirhart +3 more
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Cloning of a human ether‐a‐go‐go potassium channel expressed in myoblasts at the onset of fusion [PDF]
An early sign of human myoblast commitment to fusion is the expression of a non‐inactivating delayed rectifier K+ current, IK(NI), and an associated membrane potential hyperpolarization. We have isolated the full‐length coding region of a human ether‐a‐go‐go K+ channel (h‐eag) from myoblasts undergoing differentiation.
Teresa Occhiodoro +6 more
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Sphingosine 1-phosphate and human ether-a′-go-go-related gene potassium channels modulate migration in human anaplastic thyroid cancer cells [PDF]
Anaplastic thyroid cancer (ATC) is the most aggressive form of human thyroid cancer, lacking any effective treatment. Sphingosine 1-phosphate (S1P) receptors and human ether-a′-go-go-related gene (HERG (KCNH2)) potassium channels are important modulators of cell migration. In this study, we have shown that the S1P1–3 receptors are expressed in C643 and
Muhammad Yasir Asghar +3 more
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The Colombian scorpion Centruroides margaritatus produces a venom considered of low toxicity. Nevertheless, there are known cases of envenomation resulting in cardiovascular disorders, probably due to venom components that target ion channels. Among them,
José Beltrán-Vidal +7 more
doaj +1 more source

