1lgl: Difference between revisions

<StructureSection load='1lgl' size='340' side='right'caption='[[1lgl]]' scene=''>

<table><tr><td colspan='2'>[[1lgl]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/Mesobuthus_eupeus Mesobuthus eupeus]. Full experimental information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1LGL OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=1LGL FirstGlance]. <br>

</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">Solution NMR, 20 models</td></tr>

<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=1lgl FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1lgl OCA], [https://pdbe.org/1lgl PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=1lgl RCSB], [https://www.ebi.ac.uk/pdbsum/1lgl PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=1lgl ProSAT]</span></td></tr>

[https://www.uniprot.org/uniprot/KGX21_MESEU KGX21_MESEU] Blocks human and/or rat Kv11.1/KCNH2/ERG1, Kv11.2/KCNH6/ERG2 and Kv11.3/KCNH7/ERG3 by binding to channel outer vestibule (S5P domain) with a 1:1 stoichiometry. Inhibition data are the following: hERG1 (reversible, Kd=7.7 nM (PubMed:16497878), IC(50)=3.3 nM (PubMed:11136720), IC(50)=11.9 nM (PubMed:21205913)), rERG1 (reversible, Kd=19 nM) (PubMed:16497878), hERG2 (reversible, Kd=77 nM) (PubMed:16497878), rERG2 (irreversible, Kd=4.2 nM) (PubMed:16497878), hERG3 (reversible, Kd=11.5 nM) (PubMed:16497878) and rERG3 (reversible, Kd=747 nM) (PubMed:16497878) potassium channels. Has also a minimal effect on rat ELK1/KCNH4 potassium channels (9% inhibition at 100 nM (PubMed:15137031)). Both this toxin and CnErgTx1 (AC Q86QT3) share mechanism of action and have overlapping binding sites on ERG1 (PubMed:12719233). The potency of these two toxins is not affected by elevating potassium ion concentration from 2 to 98 mM (PubMed:12719233). In addition, at high toxin concentrations, block of ERG1 macroscopic currents by these two toxins is incomplete (88%) (PubMed:12719233). The blockade by this toxin is preferentially closed channel state-dependent, with a component of open, but not inactive state-dependent blockade (PubMed:12860380). This toxin produces a concentration-dependent prolongation of QTc in the isolated rabbit heart (16.3% at 100 nM) (PubMed:21205913).<ref>PMID:11136720</ref> <ref>PMID:12719233</ref> <ref>PMID:12860380</ref> <ref>PMID:16497878</ref> <ref>PMID:21205913</ref> <ref>PMID:8617371</ref>  

*[[Potassium channel toxin 3D structures|Potassium channel toxin 3D structures]]

[[Category: Angelo K]]

[[Category: Arseniev AS]]

[[Category: Bocharov EV]]

[[Category: Grinenko OV]]

[[Category: Grishin EV]]

[[Category: Korolokova YV]]

[[Category: Lipkin AV]]

[[Category: Maslennikov IV]]

[[Category: Nosireva ED]]

[[Category: Olesen S-P]]

[[Category: Pluzhnikov KA]]