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6ena
From Proteopedia
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| - | '''Unreleased structure''' | ||
| - | + | ==Nemertide alpha-1== | |
| - | + | <StructureSection load='6ena' size='340' side='right'caption='[[6ena]]' scene=''> | |
| - | + | == Structural highlights == | |
| - | + | <table><tr><td colspan='2'>[[6ena]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/Lineus_longissimus Lineus longissimus]. Full experimental information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6ENA OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=6ENA FirstGlance]. <br> | |
| - | + | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=HYP:4-HYDROXYPROLINE'>HYP</scene></td></tr> | |
| - | [[Category: | + | <tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=6ena FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6ena OCA], [https://pdbe.org/6ena PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=6ena RCSB], [https://www.ebi.ac.uk/pdbsum/6ena PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=6ena ProSAT]</span></td></tr> |
| + | </table> | ||
| + | == Function == | ||
| + | [https://www.uniprot.org/uniprot/NEMA1_LINLO NEMA1_LINLO] Highly potent toxin against insect sodium channel (Nav) and with less potent activity against mammalian sodium channels (PubMed:29567943). Potently inhibits inactivation of insect sodium channels of B.germanica (BgNav1) (EC(50)=8.6 nM), D.melanogaster (DmNav1), and arachnid sodium channel V.destructor (VdNav1) (PubMed:29567943, PubMed:34445875). Also delays the inactivation of most mammalian Nav channels tested (hNav1.1/SCN1A; EC(50)=124.1 nM, rNav1.2/SCN2A; EC(50)=359.6 nM, rNav1.3/SCN3A; EC(50)=135.4 nM, rNav1.4/SCN4A; EC(50)=145.5 nM, hNav1.5/SCN5A; EC(50)=138.3 nM, mNav1.6/SCN8A; EC(50)=240.4 nM, hNav1.9/SCN9A; EC(50)=76.5 nM) (PubMed:29567943, PubMed:34445875). 1 uM is enough to completely inhibits the inactivation, resulting in sustained non-inactivating currents (PubMed:29567943). In addition, the toxin significantly enhances the recovery from inactivation, and the open state is not required for the toxin to interact with the channel (PubMed:29567943). In vivo, injection into green crabs (Carcinus maenas at 1 mug/kg) of small doses (1-5 ug/kg) results in slow and fast permanent paralysis, whereas injection of high doses (more than 10 ug/kg) causes death (PubMed:29567943). Injection into juvenile Blaptica dubia cockroaches results in death or permanent paralysis at doses higher than 7.1 ug/kg (PubMed:29567943). Injection into brine shrimp (Artemia salina) stops movement or causes death after 24 hours (EC(50)=0.3 uM) (PubMed:34445875). In the rare inherited cardiac arrhythmia Brugada syndrome 1 (BRGDA1), this toxin is able to restore the loss of function by reducing channel inactivation, without affecting activation, by binding to Nav1.5/SCN5A (PubMed:32850980).<ref>PMID:29567943</ref> <ref>PMID:32850980</ref> <ref>PMID:34445875</ref> | ||
| + | == References == | ||
| + | <references/> | ||
| + | __TOC__ | ||
| + | </StructureSection> | ||
| + | [[Category: Large Structures]] | ||
| + | [[Category: Lineus longissimus]] | ||
| + | [[Category: Goransson U]] | ||
| + | [[Category: Jacobsson E]] | ||
| + | [[Category: Rosengren KJ]] | ||
Current revision
Nemertide alpha-1
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