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1lgl

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{{STRUCTURE_1lgl| PDB=1lgl | SCENE= }}
 
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===Solution structure of HERG-specific scorpion toxin BeKm-1===
 
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{{ABSTRACT_PUBMED_12151390}}
 
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==About this Structure==
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==Solution structure of HERG-specific scorpion toxin BeKm-1==
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[[1lgl]] is a 1 chain structure with sequence from [http://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].
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<StructureSection load='1lgl' size='340' side='right'caption='[[1lgl]]' scene=''>
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== Structural highlights ==
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<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>
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</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">Solution NMR</td></tr>
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<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>
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</table>
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== Function ==
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[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>
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<div style="background-color:#fffaf0;">
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== Publication Abstract from PubMed ==
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The scorpion toxin BeKm-1 is unique among a variety of known short scorpion toxins affecting potassium channels in its selective action on ether-a-go-go-related gene (ERG)-type channels. BeKm-1 shares the common molecular scaffold with other short scorpion toxins. The toxin spatial structure resolved by NMR consists of a short alpha-helix and a triple-stranded antiparallel beta-sheet. By toxin mutagenesis study we identified the residues that are important for the binding of BeKm-1 to the human ERG K+ (HERG) channel. The most critical residues (Tyr-11, Lys-18, Arg-20, Lys-23) are located in the alpha-helix and following loop whereas the "traditional" functional site of other short scorpion toxins is formed by residues from the beta-sheet. Thus the unique location of the binding site of BeKm-1 provides its specificity toward the HERG channel.
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==See Also==
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New binding site on common molecular scaffold provides HERG channel specificity of scorpion toxin BeKm-1.,Korolkova YV, Bocharov EV, Angelo K, Maslennikov IV, Grinenko OV, Lipkin AV, Nosyreva ED, Pluzhnikov KA, Olesen SP, Arseniev AS, Grishin EV J Biol Chem. 2002 Nov 8;277(45):43104-9. Epub 2002 Jul 31. PMID:12151390<ref>PMID:12151390</ref>
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*[[Potassium channel toxin|Potassium channel toxin]]
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==Reference==
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From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
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<ref group="xtra">PMID:012151390</ref><references group="xtra"/>
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</div>
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<div class="pdbe-citations 1lgl" style="background-color:#fffaf0;"></div>
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==See Also==
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*[[Potassium channel toxin 3D structures|Potassium channel toxin 3D structures]]
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== References ==
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<references/>
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__TOC__
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</StructureSection>
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[[Category: Large Structures]]
[[Category: Mesobuthus eupeus]]
[[Category: Mesobuthus eupeus]]
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[[Category: Angelo, K.]]
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[[Category: Angelo K]]
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[[Category: Arseniev, A S.]]
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[[Category: Arseniev AS]]
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[[Category: Bocharov, E V.]]
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[[Category: Bocharov EV]]
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[[Category: Grinenko, O V.]]
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[[Category: Grinenko OV]]
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[[Category: Grishin, E V.]]
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[[Category: Grishin EV]]
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[[Category: Korolokova, Y V.]]
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[[Category: Korolokova YV]]
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[[Category: Lipkin, A V.]]
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[[Category: Lipkin AV]]
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[[Category: Maslennikov, I V.]]
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[[Category: Maslennikov IV]]
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[[Category: Nosireva, E D.]]
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[[Category: Nosireva ED]]
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[[Category: Olesen, S P.]]
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[[Category: Olesen S-P]]
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[[Category: Pluzhnikov, K A.]]
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[[Category: Pluzhnikov KA]]
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[[Category: Alpha-beta motif]]
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[[Category: Cysteine-knot motif]]
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[[Category: Toxin]]
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Current revision

Solution structure of HERG-specific scorpion toxin BeKm-1

PDB ID 1lgl

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