View source for 2m3i


==Characterization of a Novel Alpha4/6-Conotoxin TxIC from Conus textile that Potently Blocks alpha3beta4 Nicotinic Acetylcholine Receptors==
<StructureSection load='2m3i' size='340' side='right'caption='[[2m3i]]' scene=''>
== Structural highlights ==
<table><tr><td colspan='2'>[[2m3i]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/Conus_lividus Conus lividus]. Full experimental information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2M3I OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=2M3I 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='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=NH2:AMINO+GROUP'>NH2</scene></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=2m3i FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2m3i OCA], [https://pdbe.org/2m3i PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=2m3i RCSB], [https://www.ebi.ac.uk/pdbsum/2m3i PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=2m3i ProSAT]</span></td></tr>
</table>
== Function ==
[https://www.uniprot.org/uniprot/CA112_CONLI CA112_CONLI] Alpha-conotoxins act on postsynaptic membranes, they bind to the nicotinic acetylcholine receptors (nAChR) and thus inhibit them. This toxin inhibits alpha-3-beta-4, alpha-6/alpha-3-beta-4, and alpha-2-beta-4 nAChRs.[UniProtKB:K8DWB5]
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== Publication Abstract from PubMed ==
The alpha3beta4 nAChRs are implicated in pain sensation in the PNS and addiction to nicotine in the CNS. We identified an alpha-4/6-conotoxin (CTx) TxID from Conus textile. The new toxin consists of 15 amino acid residues with two disulfide bonds. TxID was synthesized using solid phase methods, and the synthetic peptide was functionally tested on nAChRs heterologously expressed in Xenopus laevis oocytes. TxID blocked rat alpha3beta4 nAChRs with a 12.5 nM IC50, which places it among the most potent alpha3beta4 nAChR antagonists. TxID also blocked the closely related alpha6/alpha3beta4 with a 94 nM IC50 but showed little activity on other nAChR subtypes. NMR analysis showed that two major structural isomers exist in solution, one of which adopts a regular alpha-CTx fold but with different surface charge distribution to other 4/6 family members. alpha-CTx TxID is a novel tool with which to probe the structure and function of alpha3beta4 nAChRs.

Characterization of a Novel alpha-Conotoxin TxID from Conus textile That Potently Blocks Rat alpha3beta4 Nicotinic Acetylcholine Receptors.,Luo S, Zhangsun D, Zhu X, Wu Y, Hu Y, Christensen S, Harvey PJ, Akcan M, Craik DJ, McIntosh JM J Med Chem. 2013 Nov 22. PMID:24200193<ref>PMID:24200193</ref>

From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
</div>
<div class="pdbe-citations 2m3i" style="background-color:#fffaf0;"></div>
== References ==
<references/>
__TOC__
</StructureSection>
[[Category: Conus lividus]]
[[Category: Large Structures]]
[[Category: Akcan M]]
[[Category: Christensen S]]
[[Category: Craik DJ]]
[[Category: Hu Y]]
[[Category: Luo S]]
[[Category: McIntosh JM]]
[[Category: Wu Y]]
[[Category: Zhangsun D]]
[[Category: Zhu X]]