Results 41 to 50 of about 115,275 (296)

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, A Vagin, AJ McCoy, AM Powl, AM Waterhouse, AO O’Reilly, D Ren, D Shaya, DA Doyle, DP Klose, E Blanc, EC McCusker, GM Clayton, IH van Stokkum, J Payandeh, JD Thompson, JG Lees, JG Lees, K Charalambous, K Irie, L Whitmore, M Petrek, M Strong, NA Baker, P Emsley, R Koishi, RA Laskowski, RM Keegan, SB Long, VB Chen, W Kabsch, W Kabsch, Y Zhao, Y Zhao   +33 more
core   +2 more sources

Inhibition of voltage-gated sodium channels by sumatriptan bioisosteres

Frontiers in Pharmacology, 2015
Voltage-gated sodium channels are known to play a pivotal role in perception and transmission of pain sensations. Gain-of-function mutations in the genes encoding the peripheral neuronal sodium channels, hNav1.7-1.9, cause human painful diseases.
Roberta eCarbonara, Alessia eCarocci, Julien eRoussel, Giuseppe eCrescenzo, Canio eBuonavoglia, Carlo eFranchini, Giovanni eLentini, Diana eConte Camerino, Jean-François eDesaphy   +8 more
doaj   +1 more source

Ionic selectivity and thermal adaptations within the voltage-gated sodium channel family of alkaliphilic Bacillus [PDF]

, 2014
Entry and extrusion of cations are essential processes in living cells. In alkaliphilic prokaryotes, high external pH activates voltage-gated sodium channels (Nav), which allows Na+ to enter and be used as substrate for cation/proton antiporters ...
Clapham, David E, DeCaen, Paul G, Ito, Masahiro, Krulwich, Terry A, Takahashi, Yuka   +4 more
core   +2 more sources

Voltage-gated sodium channels in taste bud cells

BMC Neuroscience, 2009
Background Taste bud cells transmit information regarding the contents of food from taste receptors embedded in apical microvilli to gustatory nerve fibers innervating basolateral membranes.
Williams Mark E, Kalabat Dalia, Laita Bianca, Echeverri Fernando, Lu Min, Gao Na, Hevezi Peter, Zlotnik Albert, Moyer Bryan D   +8 more
doaj   +1 more source

Structural Advances in Voltage-Gated Sodium Channels

Frontiers in Pharmacology, 2022
Voltage-gated sodium (NaV) channels are responsible for the rapid rising-phase of action potentials in excitable cells. Over 1,000 mutations in NaV channels are associated with human diseases including epilepsy, periodic paralysis, arrhythmias and pain disorders.
Daohua Jiang, Daohua Jiang, Jiangtao Zhang, Jiangtao Zhang, Zhanyi Xia, Zhanyi Xia   +5 more
openaire   +3 more sources

Cell surface interactome analysis identifies TSPAN4 as a negative regulator of PD‐L1 in melanoma

Molecular Oncology, EarlyView.
Using cell surface proximity biotinylation, we identified tetraspanin TSPAN4 within the PD‐L1 interactome of melanoma cells. TSPAN4 negatively regulates PD‐L1 expression and lateral mobility by limiting its interaction with CMTM6 and promoting PD‐L1 degradation.
Guus A. Franken, Andrea Abel Gutierrez, Imke van Rossum, Cornelia G. Spruijt, Michiel Vermeulen, Guido van Mierlo, Blanca Scheijen, Annemiek B. van Spriel   +7 more
wiley   +1 more source

Potential roles of voltage-gated ion channel disruption in Tuberous Sclerosis Complex

Frontiers in Molecular Neuroscience
Tuberous 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, Roy E. Strowd III, Kimberly F. Raab-Graham   +2 more
doaj   +1 more source

Photocontrol of Voltage-Gated Ion Channel Activity by Azobenzene Trimethylammonium Bromide in Neonatal Rat Cardiomyocytes. [PDF]

PLoS ONE, 2016
The ability of azobenzene trimethylammonium bromide (azoTAB) to sensitize cardiac tissue excitability to light was recently reported. The dark, thermally relaxed trans- isomer of azoTAB suppressed spontaneous activity and excitation propagation speed ...
Sheyda R Frolova, Olga Gaiko, Valeriya A Tsvelaya, Oleg Y Pimenov, Konstantin I Agladze   +4 more
doaj   +1 more source

Strategies for studying permeation at voltage-gated ion channels [PDF]

, 1991
Voltage-dependent ion channels are presently thought to consist of several distinct functional regions: (a) activation gates, (b) inactivation gates, and permeation pathways.
Lester, Henry A.
core   +1 more source

The PI3Kδ inhibitor roginolisib (IOA‐244) preserves T‐cell function and activity

Molecular Oncology, EarlyView.
Identification of novel PI3K inhibitors with limited immune‐related adverse effects is highly sought after. We found that roginolisib and idelalisib inhibit chronic lymphocytic leukemia (CLL) cells and Treg suppressive functions to similar extents, but roginolisib affects cytotoxic T‐cell function and promotion of pro‐inflammatory T helper subsets to a
Elise Solli, Alessio Bevilacqua, Mathias Wenes, Denis Migliorini, Lars van der Veen, Sigrid S Skånland, Giusy Di Conza, Kjetil Taskén   +7 more
wiley   +1 more source