Voltage-gated sodium channels: biophysics, pharmacology, and related channelopathies
Frontiers in Pharmacology, 2012 Voltage-gated sodium channels (VGSC) are multi-molecular protein complexes expressed in both excitable and non-excitable cells. They are primarily formed by a pore-forming multi-spanning integral membrane glycoprotein (α-subunit) that can be associated ...
Eleonora eSavio Galimberti +2 more
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High-threshold mechanosensitive ion channels blocked by a novel conopeptide mediate pressure-evoked pain [PDF]
, 2007 Little is known about the molecular basis of somatosensory mechanotransduction in mammals. We screened a library of peptide toxins for effects on mechanically activated currents in cultured dorsal root ganglion neurons.
Abrahamsen, B +11 more
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Structure of a bacterial voltage-gated sodium channel pore reveals mechanisms of opening and closing [PDF]
, 2012 Voltage-gated sodium channels are vital membrane proteins essential for electrical signalling; in humans, they are key targets for the development of pharmaceutical drugs. Here we report the crystal structure of an open-channel conformation of NavMs, the
A Lampert +33 more
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Voltage-gated sodium channels dysfunction in depression: the hypothesis
Psychiatry and Behavioral Sciences, 2016 Voltage-gated sodium (Na+) channels (VGSCs) are responsible for action potential initiation and propagation in most electrically excitable cells which are implicated in a wide range physiological functions including neuronal signalling, muscle ...
Osman Ozdemir
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Searching for New Leads to Treat Epilepsy: Target-Based Virtual Screening for the Discovery of Anticonvulsant Agents [PDF]
, 2018 The purpose of this investigation is to contribute to the development of new anticonvulsant drugs to treat patients with refractory epilepsy. We applied a virtual screening protocol that involved the search into molecular databases of new compounds and ...
Bruno Blanch, Luis Enrique +8 more
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Potential roles of voltage-gated ion channel disruption in Tuberous Sclerosis Complex
Frontiers in Molecular NeuroscienceTuberous Sclerosis Complex (TSC) is a lynchpin disorder, as it results in overactive mammalian target of rapamycin (mTOR) signaling, which has been implicated in a multitude of disease states.
Hailey X. Egido-Betancourt +2 more
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Voltage-Gated Sodium Channels as Insecticide Targets [PDF]
, 2014 Voltage-gated sodium channels are critical for the generation and propagation of action potentials. They are the primary target of several classes of insecticides, including DDT, pyrethroids and sodium channel blocker insecticides (SCBIs). DDT and pyrethroids preferably bind to open sodium channels and stabilize the open state, causing prolonged ...
Kristopher S, Silver +6 more
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Structural modeling of ion channels using AlphaFold2, RoseTTAFold2, and ESMFold
ChannelsIon channels play key roles in human physiology and are important targets in drug discovery. The atomic-scale structures of ion channels provide invaluable insights into a fundamental understanding of the molecular mechanisms of channel gating and ...
Phuong Tran Nguyen +5 more
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Propranolol blocks cardiac and neuronal voltage-gated sodium channels
Frontiers in Pharmacology, 2010 Propranolol is a widely-used, nonselective ß-adrenergic receptor antagonist with proven efficacy in treating cardiovascular disorders and in the prevention of migraine headaches.
Dao W Wang +7 more
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Noncanonical Roles of Voltage-Gated Sodium Channels
Neuron, 2013 The Hodgkin-Huxley formulation, at its 60th anniversary, remains a bastion of neuroscience. Sodium channels Nav1.1-Nav1.3 and Nav1.6-Nav1.9 support electrogenesis in neurons and are often considered "neuronal," whereas Nav1.4 and Nav1.5 drive electrogenesis in skeletal and cardiac muscle.
Black, Joel A., Waxman, Stephen G.
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