6sxc
From Proteopedia
(Difference between revisions)
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==Crystal structure of the Voltage-Gated Sodium Channel NavMs (F208L) in complex with 4-hydroxytamoxifen (2.5 Angstrom resolution)== | ==Crystal structure of the Voltage-Gated Sodium Channel NavMs (F208L) in complex with 4-hydroxytamoxifen (2.5 Angstrom resolution)== | ||
| - | <StructureSection load='6sxc' size='340' side='right'caption='[[6sxc]]' scene=''> | + | <StructureSection load='6sxc' size='340' side='right'caption='[[6sxc]], [[Resolution|resolution]] 2.50Å' scene=''> |
== Structural highlights == | == Structural highlights == | ||
| - | <table><tr><td colspan='2'>Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6SXC OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=6SXC FirstGlance]. <br> | + | <table><tr><td colspan='2'>[[6sxc]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/Magnetococcus_marinus_MC-1 Magnetococcus marinus MC-1]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6SXC OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=6SXC 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=6sxc FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6sxc OCA], [https://pdbe.org/6sxc PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=6sxc RCSB], [https://www.ebi.ac.uk/pdbsum/6sxc PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=6sxc ProSAT]</span></td></tr> | + | </td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 2.5Å</td></tr> |
| + | <tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=12P:DODECAETHYLENE+GLYCOL'>12P</scene>, <scene name='pdbligand=2CV:HEGA-10'>2CV</scene>, <scene name='pdbligand=NA:SODIUM+ION'>NA</scene>, <scene name='pdbligand=OHT:4-HYDROXYTAMOXIFEN'>OHT</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=6sxc FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6sxc OCA], [https://pdbe.org/6sxc PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=6sxc RCSB], [https://www.ebi.ac.uk/pdbsum/6sxc PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=6sxc ProSAT]</span></td></tr> | ||
</table> | </table> | ||
| + | == Function == | ||
| + | [https://www.uniprot.org/uniprot/A0L5S6_MAGMM A0L5S6_MAGMM] | ||
| + | <div style="background-color:#fffaf0;"> | ||
| + | == Publication Abstract from PubMed == | ||
| + | Voltage-gated sodium channels are targets for many analgesic and antiepileptic drugs whose therapeutic mechanisms and binding sites have been well characterized. We describe the identification of a previously unidentified receptor site within the NavMs voltage-gated sodium channel. Tamoxifen, an estrogen receptor modulator, and its primary and secondary metabolic products bind at the intracellular exit of the channel, which is a site that is distinct from other previously characterized sodium channel drug sites. These compounds inhibit NavMs and human sodium channels with similar potencies and prevent sodium conductance by delaying channel recovery from the inactivated state. This study therefore not only describes the structure and pharmacology of a site that could be leveraged for the development of new drugs for the treatment of sodium channelopathies but may also have important implications for off-target health effects of this widely used therapeutic drug. | ||
| + | |||
| + | A tamoxifen receptor within a voltage-gated sodium channel.,Sula A, Hollingworth D, Ng LCT, Larmore M, DeCaen PG, Wallace BA Mol Cell. 2021 Mar 18;81(6):1160-1169.e5. doi: 10.1016/j.molcel.2020.12.048. Epub , 2021 Jan 26. PMID:33503406<ref>PMID:33503406</ref> | ||
| + | |||
| + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | ||
| + | </div> | ||
| + | <div class="pdbe-citations 6sxc" style="background-color:#fffaf0;"></div> | ||
| + | |||
| + | ==See Also== | ||
| + | *[[Ion channels 3D structures|Ion channels 3D structures]] | ||
| + | == References == | ||
| + | <references/> | ||
__TOC__ | __TOC__ | ||
</StructureSection> | </StructureSection> | ||
[[Category: Large Structures]] | [[Category: Large Structures]] | ||
| + | [[Category: Magnetococcus marinus MC-1]] | ||
[[Category: Hollingworth D]] | [[Category: Hollingworth D]] | ||
[[Category: Sula A]] | [[Category: Sula A]] | ||
[[Category: Wallace BA]] | [[Category: Wallace BA]] | ||
Current revision
Crystal structure of the Voltage-Gated Sodium Channel NavMs (F208L) in complex with 4-hydroxytamoxifen (2.5 Angstrom resolution)
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