2n27: Difference between revisions
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==Direct attack of vanilloids on the regulation of the pain receptor TRPV1== | |||
<StructureSection load='2n27' size='340' side='right' caption='[[2n27]], [[NMR_Ensembles_of_Models | 20 NMR models]]' scene=''> | |||
== Structural highlights == | |||
<table><tr><td colspan='2'>[[2n27]] is a 1 chain structure. Full experimental information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2N27 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2N27 FirstGlance]. <br> | |||
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=4DY:(6E)-N-(4-HYDROXY-3-METHOXYBENZYL)-8-METHYLNON-6-ENAMIDE'>4DY</scene>, <scene name='pdbligand=CA:CALCIUM+ION'>CA</scene></td></tr> | |||
<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2n27 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2n27 OCA], [http://pdbe.org/2n27 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=2n27 RCSB], [http://www.ebi.ac.uk/pdbsum/2n27 PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=2n27 ProSAT]</span></td></tr> | |||
</table> | |||
<div style="background-color:#fffaf0;"> | |||
== Publication Abstract from PubMed == | |||
There is enormous interest toward vanilloid agonists of the pain receptor TRPV1 in analgesic therapy, but the mechanisms of their sensory neuron-blocking effects at high or repeated doses are still a matter of debate. Our results have demonstrated that capsaicin and resiniferatoxin form nanomolar complexes with calmodulin, and competitively inhibit TRPV1-calmodulin interaction. These interactions involve the protein recognition interface of calmodulin, which is responsible for all of the cell-regulatory calmodulin-protein interactions. These results draw attention to a previously unknown vanilloid target, which may contribute to the explanation of the paradoxical pain-modulating behaviour of these important pharmacons. This article is protected by copyright. All rights reserved. | |||
Competitive inhibition of TRPV1 - calmodulin interaction by vanilloids.,Hetenyi A, Nemeth L, Weber E, Szakonyi G, Winter Z, Josvay K, Bartus E, Olah Z, Martinek TA FEBS Lett. 2016 Jun 24. doi: 10.1002/1873-3468.12267. PMID:27339229<ref>PMID:27339229</ref> | |||
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |||
</div> | |||
[[Category: | <div class="pdbe-citations 2n27" style="background-color:#fffaf0;"></div> | ||
== References == | |||
<references/> | |||
__TOC__ | |||
</StructureSection> | |||
[[Category: Hetenyi, A]] | |||
[[Category: Josvay, K]] | [[Category: Josvay, K]] | ||
[[Category: | [[Category: Martinek, T A]] | ||
[[Category: Nemeth, L]] | [[Category: Nemeth, L]] | ||
[[Category: Olah, Z]] | |||
[[Category: Szakonyi, G]] | [[Category: Szakonyi, G]] | ||
[[Category: | [[Category: Weber, E]] | ||
[[Category: | [[Category: Winter, Z]] | ||
[[Category: Calmodulin]] | |||
[[Category: Capsaicin]] | |||
[[Category: Metal binding protein]] | |||
