View source for 2k4u


==Solution structure of the SCORPION TOXIN ADWX-1==
<StructureSection load='2k4u' size='340' side='right'caption='[[2k4u]], [[NMR_Ensembles_of_Models | 20 NMR models]]' scene=''>
== Structural highlights ==
<table><tr><td colspan='2'>[[2k4u]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/Buthus_martensi Buthus martensi]. Full experimental information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2K4U OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=2K4U FirstGlance]. <br>
</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=2k4u FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2k4u OCA], [https://pdbe.org/2k4u PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=2k4u RCSB], [https://www.ebi.ac.uk/pdbsum/2k4u PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=2k4u ProSAT]</span></td></tr>
</table>
== Function ==
[[https://www.uniprot.org/uniprot/KAX36_MESMA KAX36_MESMA]] Blocks voltage-gated potassium channels. At 2 uM, blocks rat Kv1.1/KCNA1 and Kv1.3/KCNA3, has a strong effect on rat Kv1.2/KCNA2 and Kv1.6/KCNA6 as well as a moderate effect on Shaker IR.<ref>PMID:9354615</ref> <ref>PMID:20713119</ref>  
== Evolutionary Conservation ==
[[Image:Consurf_key_small.gif|200px|right]]
Check<jmol>
  <jmolCheckbox>
    <scriptWhenChecked>; select protein; define ~consurf_to_do selected; consurf_initial_scene = true; script "/wiki/ConSurf/k4/2k4u_consurf.spt"</scriptWhenChecked>
    <scriptWhenUnchecked>script /wiki/extensions/Proteopedia/spt/initialview01.spt</scriptWhenUnchecked>
    <text>to colour the structure by Evolutionary Conservation</text>
  </jmolCheckbox>
</jmol>, as determined by [http://consurfdb.tau.ac.il/ ConSurfDB]. You may read the [[Conservation%2C_Evolutionary|explanation]] of the method and the full data available from [http://bental.tau.ac.il/new_ConSurfDB/main_output.php?pdb_ID=2k4u ConSurf].
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== Publication Abstract from PubMed ==
The low selectivity of Kv1 peptide inhibitors for specific isoforms makes them poor candidates for the development of theraputics. Using combined approaches, we showed that the Kv1 turret is the critical determinant for ADWX-1 peptide inhibitor selectivity of Kv1.3 over Kv1.1. Mutation of Kv1.1 turret residues to match the sequence of Kv1.3 lead to increased inhibition of Kv1.1 activity. These studies may lead to improvements in peptide inhibitor drug development.

Different Residues in Channel Turret Determining the Selectivity of ADWX-1 Inhibitor Peptide between Kv1.1 and Kv1.3 Channels.,Yin SJ, Jiang L, Yi H, Han S, Yang DW, Liu ML, Liu H, Cao ZJ, Wu YL, Li WX J Proteome Res. 2008 Nov 7;7(11):4890-4897. Epub 2008 Oct 21. PMID:18937510<ref>PMID:18937510</ref>

From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
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<div class="pdbe-citations 2k4u" style="background-color:#fffaf0;"></div>

==See Also==
*[[Potassium channel toxin 3D structures|Potassium channel toxin 3D structures]]
== References ==
<references/>
__TOC__
</StructureSection>
[[Category: Buthus martensi]]
[[Category: Large Structures]]
[[Category: Cao, Z J]]
[[Category: Han, S]]
[[Category: Jiang, L]]
[[Category: Li, W X]]
[[Category: Liu, H]]
[[Category: Liu, M L]]
[[Category: Wu, Y L]]
[[Category: Yang, D W]]
[[Category: Yi, H]]
[[Category: Yin, S J]]
[[Category: Adwx-1 peptide selectivity]]
[[Category: Amidation]]
[[Category: Channel turret]]
[[Category: Ionic channel inhibitor]]
[[Category: Kv1 1 channel]]
[[Category: Kv1 3 channel]]
[[Category: Neurotoxin]]
[[Category: Potassium channel inhibitor]]
[[Category: Secreted]]
[[Category: Structural basis]]
[[Category: Toxin]]