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The EAG Voltage-Dependent K+ Channel Subfamily: Similarities and Differences in Structural Organization and Gating

Francisco Barros, Pilar de la Peña, Pedro Domı́nguez, L.M. Sierra, Luis A. Pardo

2020Frontiers in Pharmacology47 citationsDOIOpen Access PDF

Abstract

-type channels share a domain-swapped VSD/PD organization, with each VSD contacting the PD of the adjacent subunit. In this case, the S4-S5 linker, acting as a rigid mechanical lever (electromechanical lever coupling), would lead to channel gate opening at the cytoplasmic S6 helices bundle. However, new functional data with EAG channels split between the VSD and PD modules indicate that, in some Kv channels, alternative VSD/PD coupling mechanisms do exist. Noticeably, recent elucidation of the architecture of some EAG channels, and other relatives, showed that their VSDs are non-domain swapped. Despite similarities in primary sequence and predicted structural organization for all EAG channels, they show marked kinetic differences whose molecular basis is not completely understood. Thus, while a common general architecture may establish the gating system used by the EAG channels and the physicochemical coupling of voltage sensing to gating, subtle changes in that common structure, and/or allosteric influences of protein domains relatively distant from the central gating machinery, can crucially influence the gating process. We consider here the latest advances on these issues provided by the elucidation of eag1 and erg1 three-dimensional structures, and by both classical and more recent functional studies with different members of the EAG subfamily.

Topics & Concepts

GatingPotassium channelShakerBiophysicsChemistryMembrane potentialInward-rectifier potassium ion channelTransmembrane domainProtein subunitVoltage-gated ion channelCoupling (piping)Transmembrane proteinVoltage-gated potassium channelIon channelBiochemistryMembraneMaterials scienceBiologyPhysicsReceptorQuantum mechanicsVibrationGeneMetallurgyIon channel regulation and functionCardiac electrophysiology and arrhythmiasNeuroscience and Neuropharmacology Research
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