CrystalstructureofK+channelsMutagenesisapproacheBiophysicalapproacheX-rayanalysisThecrystalstructureofKCsAchannelprovidesthefirstthree-dimensional structure oftheconductionpore thatfits consistently with current understanding of the corefunctionality of K+ channels.The understandingof structural information can beappliedtodesignselectivecompoundstargetingKtchannels andwouldrevolutionizeand refineapproaches targeting K+channels fortherapeuticpurposes
Crystal structure of K+ channels Mutagenesis approache Biophysical approache X-ray analysis The crystal structure of KCsA channel provides the first three-dimensional structure of the conduction pore that fits consistently with current understanding of the core functionality of K+ channels. The understanding of structural information can be applied to design selective compounds targeting K+ channels and would revolutionize and refine approaches targeting K+ channels for therapeutic purposes
Overall architecture of KirchannelsExtracelularCytoplasmPorehelixOQ0Selectivityfilter-M1:outerhelixM2:innerhelixSlidehelix?Cytoplasmicpore
Overall architecture of Kir channels
Structures of the cytoplasmic domains ofKirBac1.1 and Kir3.1TM
Structures of the cytoplasmic domains of KirBac1.1 and Kir3.1
InwardrectificationStrongrectifierNormalizedcurrentWeakrectifier1.5o-Strongrectifier-Weakrectifier1.00000020μA80-4040mV0.550ms50 mV--1.0bC(μA)Control+Mg2+Spermidine2(mV)-5(3)H-aH(4)A
Inward rectification
Gating of Kir channelsbClosedaOpenSelectivityfilterGlycine134BundleGlycine143crossingd.InterburstClosedOpenBurstclosureItt.Intraburstclosures义书98.Wurhn160ms
Gating of Kir channels