[hal-01076470] Voltage-Gated Sodium Channel Blockers Library from OTAVA

Voltage-gated sodium channels are a class of large integral membrane proteins composed of a highly processed α subunit and one or several smaller β subunits The α-subunit forms ion-conducting aqueous pore whereas auxiliary β subunits modify the kinetics and voltage-dependence of channel gating Voltage-gated ion channels are implicated in the regulation of synaptic transmission muscle contraction and hormone secretion in response to membrane depolarization It was demonstrated that dysfunction of voltage-gated sodium channels led to the development of a wide range of human pathologies such as inherited epilepsy migraine periodic paralysis cardiac arrhythmia chronic pain syndromes and others Therefore the inhibition of voltage-gated sodium channels could be an effective strategy to prevent the development of these diseases OTAVA Ltd offers new Voltage-gated sodium channel blockers library containing 1630 compounds The library was designed as a special screening collection comprising compounds with predicted sodium channels blocking activity and selectivity The compounds have been selected by pharmacophore screening of OTAVA Drug-like Green Collection toward three ligand-based pharmacophore models The models were generated based on the known sodium channel blockers divided into three groups according to their structural features This library comprises drug-like compounds only and provides an excellent basis for drug discovery



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