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Page 1: Voltage-gated sodium channels (NaV

IUPHAR/BPSGuidetoPharmacologyCITEhttps://doi.org/10.2218/gtopdb/F82/2021.3

Voltage-gatedsodiumchannels(NaV)inGtoPdbv.2021.3

WilliamA.Catterall1,AlanL.Goldin2andStephenG.Waxman3

1. UniversityofWashington,USA2. UniversityofCalifornia,USA3. YaleUniversity,USA

Abstract

Sodiumchannelsarevoltage-gatedsodium-selectiveionchannelspresentinthemembraneofmostexcitablecells.Sodiumchannelscompriseofonepore-formingαsubunit,whichmaybeassociatedwitheitheroneortwoβsubunits[177].α-Subunitsconsistoffourhomologousdomains(I-IV),eachcontainingsixtransmembranesegments(S1-S6)andapore-formingloop.Thepositivelychargedfourthtransmembranesegment(S4)actsasavoltagesensorandisinvolvedinchannelgating.ThecrystalstructureofthebacterialNavAbchannelhasrevealedanumberofnovelstructuralfeaturescomparedtoearlierpotassiumchannelstructuresincludingashortselectivityfilterwithionselectivitydeterminedbyinteractionswithglutamatesidechains[274].Interestingly,theporeregionispenetratedbyfattyacylchainsthatextendintothecentralcavitywhichmayallowtheentryofsmall,hydrophobicpore-blockingdrugs[274].Auxiliaryβ1,β2,β3andβ4subunitsconsistofalargeextracellularN-terminaldomain,asingletransmembranesegmentandashortercytoplasmicdomain.

ThenomenclatureforsodiumchannelswasproposedbyGoldinetal.,(2000)[144]andapprovedbytheNC-IUPHARSubcommitteeonsodiumchannels(Catteralletal.,2005,[52]).

Contents

ThisisacitationsummaryforVoltage-gatedsodiumchannels(NaV)intheGuidetoPharmacologydatabase(GtoPdb).Itexistspurelyasanadjuncttothedatabasetofacilitatetherecognitionofcitationstoandfromthedatabasebycitationanalyzers.Readerswillalmostcertainlywanttovisittherelevantsectionsofthedatabasewhicharegivenhereunderdatabaselinks.

GtoPdbisanexpert-drivenguidetopharmacologicaltargetsandthesubstancesthatactonthem.GtoPdbisareferenceworkwhichismostusefullyrepresentedasanon-linedatabase.Asinanypublicationthisworkshouldbeappropriatelycited,andthepapersitcitesshouldalsoberecognized.Thisdocumentprovidesacitationfortherelevantpartsofthedatabase,andalsoprovidesareferencelistfortheresearchcitedbythoseparts.Forfurtherdetailssee[40].

PleasenotethatthedatabaseversionforthecitationsgiveninGtoPdbaretothemostrecentprecedingversioninwhichthefamilyoritssubfamiliesandtargetsweresubstantiallychanged.Thelinksbelowaretothecurrentversion.Ifyouneedtoconsultthecitedversion,ratherthanthemostrecentversion,pleasecontacttheGtoPdbcurators.

Databaselinks

Voltage-gatedsodiumchannels(NaV)https://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=82IntroductiontoVoltage-gatedsodiumchannels(NaV)https://www.guidetopharmacology.org/GRAC/FamilyIntroductionForward?familyId=82ChannelsandSubunitsNav1.1https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=578Nav1.2https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=579

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Nav1.3https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=580Nav1.4https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=581Nav1.5https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=582Nav1.6https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=583Nav1.7https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=584Nav1.8https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=585Nav1.9https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=586

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