Protonation state of inhibitors determines interaction sites within voltage-gated sodium channels
نویسندگان
چکیده
منابع مشابه
Voltage-Gated Sodium Channels Modulation by Bothutous Schach Scorpion Venom
Buthotus schach is one of the dangers scorpion in Iran that belong to the Buthidae family. Toxins are existing in venom scorpion, modulate the ion channels by blocking or opening the pore of the channel or by altering the voltage gating and useful as pharmacological tools. In the present study, we investigated the effect of venom and its obtained fractions by gel filtrations on electrophysiolog...
متن کاملVoltage sensor interaction site for selective small molecule inhibitors of voltage-gated sodium channels.
Voltage-gated sodium (Nav) channels play a fundamental role in the generation and propagation of electrical impulses in excitable cells. Here we describe two unique structurally related nanomolar potent small molecule Nav channel inhibitors that exhibit up to 1,000-fold selectivity for human Nav1.3/Nav1.1 (ICA-121431, IC50, 19 nM) or Nav1.7 (PF-04856264, IC50, 28 nM) vs. other TTX-sensitive or ...
متن کاملVOLTAGE-GATED ION CHANNELS Voltage-Gated Sodium Channels
Antiepileptic drugs (AEDs) protect against seizures through interactions with a variety of cellular targets. By affecting the functional activity of these targets, AEDs suppress abnormal hypersynchronous activity in brain circuits, leading to protection against seizures. The actions on these targets can be categorized into four broad groups: (i) modulation of voltage-gated ion channels, includi...
متن کاملNoncanonical Roles of Voltage-Gated Sodium Channels
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. These channels are, however, expressed in cell types that are not considered electrically excitable. Here, ...
متن کاملNomenclature of Voltage-Gated Sodium Channels
been given different names, so that there are multiple Sodium Channels synonyms for many of sodium channel isoforms. To eliminate confusion resulting from the multiplicity of names, we propose a standardized nomenclature for Voltage-gated sodium channels are critical elements of voltage-gated sodium channels (Table 1). This nomen-action potential initiation and propagation in excitable clature ...
متن کاملذخیره در منابع من
با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید
ژورنال
عنوان ژورنال: Proceedings of the National Academy of Sciences
سال: 2018
ISSN: 0027-8424,1091-6490
DOI: 10.1073/pnas.1714131115