View source for 8w16


==Pyroglutamaic acid position 1 synthetic analogue of RgIA==
<StructureSection load='8w16' size='340' side='right'caption='[[8w16]]' scene=''>
== Structural highlights ==
<table><tr><td colspan='2'>[[8w16]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/Conus_regius Conus regius]. Full experimental information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=8W16 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=8W16 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=IYR:3-IODO-TYROSINE'>IYR</scene>, <scene name='pdbligand=PCA:PYROGLUTAMIC+ACID'>PCA</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=8w16 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=8w16 OCA], [https://pdbe.org/8w16 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=8w16 RCSB], [https://www.ebi.ac.uk/pdbsum/8w16 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=8w16 ProSAT]</span></td></tr>
</table>
== Function ==
[https://www.uniprot.org/uniprot/CA1A_CONRE CA1A_CONRE] This toxin target two types of receptors, the nicotinic acetylcholine receptor (nAChR) and the G-protein-coupled receptor GABA(B). It specifically inhibits the alpha-9-alpha-10/CHRNA9-CHRNA10 nAChR, with preference for rat receptors (PubMed:16445293, PubMed:21888386, PubMed:22774872, PubMed:25740413, PubMed:28223528, PubMed:18242183, PubMed:18295795). It interacts with the alpha-10(+)/alpha-9(-)interface of the receptor (PubMed:25740413). It shows a two order of magnitude species difference potency for the rat versus human alpha-9-alpha-10 nAChR, due to the Thr-86 located in the alpha-9 nAChR subunit (PubMed:22774872). This toxin also shows inhibition of high voltage-activated (HVA) calcium channels (Cav2.2) by acting on GABA(B) receptors (GABBR1 and GABBR2) (PubMed:18945902, PubMed:21888386). In vivo, this toxin produces an acute antinociceptive effect in peripheral nerve-injured rats, which may be related to the inhibition of immune cell buildup at the site of nerve injury (PubMed:17101979). In addition, when intramuscularly injected into rats following chronic constriction injury of the sciatic nerve, this toxin protects peripheral nervous tissues as well as prevents central maladaptive plasticity by inhibiting glial cell activation (PubMed:25008370).<ref>PMID:16445293</ref> <ref>PMID:17101979</ref> <ref>PMID:18242183</ref> <ref>PMID:18295795</ref> <ref>PMID:18945902</ref> <ref>PMID:21888386</ref> <ref>PMID:22774872</ref> <ref>PMID:25008370</ref> <ref>PMID:25740413</ref> <ref>PMID:28223528</ref> 
== References ==
<references/>
__TOC__
</StructureSection>
[[Category: Conus regius]]
[[Category: Large Structures]]
[[Category: Agwa AJ]]