6vnz
From Proteopedia
(Difference between revisions)
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<StructureSection load='6vnz' size='340' side='right'caption='[[6vnz]]' scene=''> | <StructureSection load='6vnz' size='340' side='right'caption='[[6vnz]]' scene=''> | ||
== Structural highlights == | == Structural highlights == | ||
| - | <table><tr><td colspan='2'> | + | <table><tr><td colspan='2'>Full experimental information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6VNZ OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=6VNZ 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=6vnz FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6vnz OCA], [https://pdbe.org/6vnz PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=6vnz RCSB], [https://www.ebi.ac.uk/pdbsum/6vnz PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=6vnz ProSAT]</span></td></tr> | + | </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='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=6vnz FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6vnz OCA], [https://pdbe.org/6vnz PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=6vnz RCSB], [https://www.ebi.ac.uk/pdbsum/6vnz PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=6vnz ProSAT]</span></td></tr> | ||
</table> | </table> | ||
| - | == Function == | ||
| - | [https://www.uniprot.org/uniprot/KAX54_HOTTA KAX54_HOTTA] Blocks small conductance calcium-activated potassium channels (PubMed:12239213). Shows activity on KCa2.2/KCNN2 (IC(50)=0.0243 nM), KCa2.3/KCNN3 (IC(50)=1.7 nM), and KCa2.1/KCNN1 (IC(50)=42 nM) (PubMed:12239213). Induces cell death when tested on Jurkat E6-1 and human mammary breast cancer MDA-MB-231 which constituvely express KCa2.2/KCNN2, but not on human peripheral blood lymphocytes (which do not express KCa2.2/KCNN2) (PubMed:24821061).<ref>PMID:12239213</ref> | ||
| - | <div style="background-color:#fffaf0;"> | ||
| - | == Publication Abstract from PubMed == | ||
| - | Peptide-based therapy against cancer is a field of great interest for biomedical developments. Since it was shown that SK3 channels promote cancer cell migration and metastatic development, we started using these channels as targets for the development of antimetastatic drugs. Particularly, tamapin (a peptide found in the venom of the scorpion Mesobuthus tamulus) is the most specific toxin against the SK2 channel currently known. Considering this fact, we designed diverse tamapin mutants based on three different hypotheses to discover a new potent molecule to block SK3 channels. We performed in vitro studies to evaluate this new toxin derivative inhibitor of cancer cell migration. Our results can be used to generate a new tamapin-based therapy against cancer cells that express SK3 channels. | ||
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| - | Novel Blocker of Onco SK3 Channels Derived from Scorpion Toxin Tamapin and Active against Migration of Cancer Cells.,Mayorga-Flores M, Chantome A, Melchor-Meneses CM, Domingo I, Titaux-Delgado GA, Galindo-Murillo R, Vandier C, Del Rio-Portilla F ACS Med Chem Lett. 2020 Jul 10;11(8):1627-1633. doi:, 10.1021/acsmedchemlett.0c00300. eCollection 2020 Aug 13. PMID:32832033<ref>PMID:32832033</ref> | ||
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| - | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | ||
| - | </div> | ||
| - | <div class="pdbe-citations 6vnz" style="background-color:#fffaf0;"></div> | ||
==See Also== | ==See Also== | ||
*[[Potassium channel toxin 3D structures|Potassium channel toxin 3D structures]] | *[[Potassium channel toxin 3D structures|Potassium channel toxin 3D structures]] | ||
| - | == References == | ||
| - | <references/> | ||
__TOC__ | __TOC__ | ||
</StructureSection> | </StructureSection> | ||
[[Category: Large Structures]] | [[Category: Large Structures]] | ||
| - | [[Category: Mesobuthus tamulus]] | ||
[[Category: Mayorga Flores M]] | [[Category: Mayorga Flores M]] | ||
[[Category: Melchor Meneses CM]] | [[Category: Melchor Meneses CM]] | ||
[[Category: Del Rio Portilla F]] | [[Category: Del Rio Portilla F]] | ||
Current revision
NMR solution structure of tamapin, mutant K20A
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