6u84
From Proteopedia
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| - | '''Unreleased structure''' | ||
| - | + | ==Apo full-length rat TRPV2 in nanodiscs, state 1== | |
| + | <StructureSection load='6u84' size='340' side='right'caption='[[6u84]], [[Resolution|resolution]] 3.70Å' scene=''> | ||
| + | == Structural highlights == | ||
| + | <table><tr><td colspan='2'>[[6u84]] is a 4 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6U84 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6U84 FirstGlance]. <br> | ||
| + | </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=6u84 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6u84 OCA], [http://pdbe.org/6u84 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6u84 RCSB], [http://www.ebi.ac.uk/pdbsum/6u84 PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6u84 ProSAT]</span></td></tr> | ||
| + | </table> | ||
| + | == Function == | ||
| + | [[http://www.uniprot.org/uniprot/TRPV2_RAT TRPV2_RAT]] Calcium-permeable, non-selective cation channel with an outward rectification. Seems to be regulated, at least in part, by growth factors, like IGF1, PDGF and morphogenetic neuropeptide/head activator. May transduce physical stimuli in mast cells. Activated by temperatures higher than 52 degrees Celsius; is not activated by vanilloids and acidic pH (By similarity).<ref>PMID:10201375</ref> <ref>PMID:15249591</ref> | ||
| + | <div style="background-color:#fffaf0;"> | ||
| + | == Publication Abstract from PubMed == | ||
| + | Transient receptor potential vanilloid 2 (TRPV2) plays a critical role in neuronal development, cardiac function, immunity, and cancer. Cannabidiol (CBD), the non-psychotropic therapeutically active ingredient of Cannabis sativa, is an activator of TRPV2 and also modulates other transient receptor potential (TRP) channels. Here, we determined structures of the full-length rat TRPV2 channel in apo and CBD-bound states in nanodiscs by cryo-electron microscopy. We show that CBD interacts with TRPV2 through a hydrophobic pocket located between S5 and S6 helices of adjacent subunits, which differs from known ligand and lipid binding sites in other TRP channels. CBD-bound TRPV2 structures revealed that the S4-S5 linker plays a critical role in channel gating upon CBD binding. Additionally, nanodiscs permitted us to visualize two distinct TRPV2 apo states in a lipid environment. Together these results provide a foundation to further understand TRPV channel gating, their divergent physiological functions, and to accelerate structure-based drug design. | ||
| - | + | Molecular mechanism of TRPV2 channel modulation by cannabidiol.,Pumroy RA, Samanta A, Liu Y, Hughes TE, Zhao S, Yudin Y, Rohacs T, Han S, Moiseenkova-Bell VY Elife. 2019 Sep 30;8. pii: 48792. doi: 10.7554/eLife.48792. PMID:31566564<ref>PMID:31566564</ref> | |
| - | + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |
| - | [[Category: | + | </div> |
| + | <div class="pdbe-citations 6u84" style="background-color:#fffaf0;"></div> | ||
| + | == References == | ||
| + | <references/> | ||
| + | __TOC__ | ||
| + | </StructureSection> | ||
| + | [[Category: Large Structures]] | ||
| + | [[Category: Moiseenkova-Bell, V Y]] | ||
| + | [[Category: Pumroy, R A]] | ||
| + | [[Category: Cannabidiol]] | ||
| + | [[Category: Ion channel]] | ||
| + | [[Category: Transport protein]] | ||
| + | [[Category: Trp channel]] | ||
| + | [[Category: Trpv2]] | ||
Revision as of 06:05, 16 October 2019
Apo full-length rat TRPV2 in nanodiscs, state 1
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