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2mdq
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==A Novel 4/7-Conotoxin LvIA from Conus lividus that Selectively Blocks 3 2 vs. 6/3 2 3 Nicotinic Acetylcholine Receptors== | ==A Novel 4/7-Conotoxin LvIA from Conus lividus that Selectively Blocks 3 2 vs. 6/3 2 3 Nicotinic Acetylcholine Receptors== | ||
| - | <StructureSection load='2mdq' size='340' side='right' caption='[[2mdq | + | <StructureSection load='2mdq' size='340' side='right'caption='[[2mdq]]' scene=''> |
== Structural highlights == | == Structural highlights == | ||
| - | <table><tr><td colspan='2'>[[2mdq]] is a 1 chain structure. Full experimental information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2MDQ OCA]. For a <b>guided tour on the structure components</b> use [ | + | <table><tr><td colspan='2'>[[2mdq]] 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=2MDQ OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=2MDQ FirstGlance]. <br> |
| - | </td></tr><tr id=' | + | </td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">Solution NMR</td></tr> |
| - | <tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[ | + | <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=2mdq FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2mdq OCA], [https://pdbe.org/2mdq PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=2mdq RCSB], [https://www.ebi.ac.uk/pdbsum/2mdq PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=2mdq ProSAT]</span></td></tr> | ||
</table> | </table> | ||
== Function == | == Function == | ||
| - | [ | + | [https://www.uniprot.org/uniprot/CA1A_CONLI CA1A_CONLI] Alpha-conotoxins act on postsynaptic membranes, they bind to the nicotinic acetylcholine receptors (nAChR) and thus inhibit them. This toxin blocks alpha-3-beta-2/CHRNA3-CHRNB2 nAChR with high selectivity (IC(50)=8.67 nM (on rat) and 17.5 (on human)) (PubMed:24398291). Has also weaker activity on alpha-6/alpha-3-beta-2-beta-3 (CHRNA6/CHRNA3-CHRNB2-CHRNB3) (IC(50)=108 nM (on rat)), alpha-6/alpha-3-beta-4 (CHRNA6/CHRNA3-CHRNB4) (IC(50)=121 nM (on rat)), alpha-3-beta-4 (CHRNA3-CHRNB4) (IC(50)=148 nM (on rat)), and alpha-7/CHRNA7 nAChRs (IC(50)=3000 nM (on rat)) (PubMed:24398291). When tested on mouse with hot-plate tests, this toxin significantly increases the base pain threshold and shows analgesic effects (PubMed:26742048).<ref>PMID:24398291</ref> <ref>PMID:26742048</ref> |
<div style="background-color:#fffaf0;"> | <div style="background-color:#fffaf0;"> | ||
== Publication Abstract from PubMed == | == Publication Abstract from PubMed == | ||
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__TOC__ | __TOC__ | ||
</StructureSection> | </StructureSection> | ||
| - | [[Category: | + | [[Category: Conus lividus]] |
| - | [[Category: | + | [[Category: Large Structures]] |
| - | [[Category: | + | [[Category: Schroeder CI]] |
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Current revision
A Novel 4/7-Conotoxin LvIA from Conus lividus that Selectively Blocks 3 2 vs. 6/3 2 3 Nicotinic Acetylcholine Receptors
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