7t37

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<StructureSection load='7t37' size='340' side='right'caption='[[7t37]], [[Resolution|resolution]] 3.70&Aring;' scene=''>
<StructureSection load='7t37' size='340' side='right'caption='[[7t37]], [[Resolution|resolution]] 3.70&Aring;' scene=''>
== Structural highlights ==
== Structural highlights ==
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<table><tr><td colspan='2'>[[7t37]] is a 4 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=7T37 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=7T37 FirstGlance]. <br>
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<table><tr><td colspan='2'>[[7t37]] is a 4 chain structure with sequence from [https://en.wikipedia.org/wiki/Rattus_norvegicus Rattus norvegicus]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=7T37 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=7T37 FirstGlance]. <br>
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</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=FZ4:2-aminoethyl+diphenylborinate'>FZ4</scene>, <scene name='pdbligand=P0T:cannabidiol'>P0T</scene></td></tr>
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</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">Electron Microscopy, [[Resolution|Resolution]] 3.7&#8491;</td></tr>
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<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=FZ4:2-aminoethyl+diphenylborinate'>FZ4</scene>, <scene name='pdbligand=P0T:cannabidiol'>P0T</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=7t37 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7t37 OCA], [https://pdbe.org/7t37 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7t37 RCSB], [https://www.ebi.ac.uk/pdbsum/7t37 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7t37 ProSAT]</span></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=7t37 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7t37 OCA], [https://pdbe.org/7t37 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7t37 RCSB], [https://www.ebi.ac.uk/pdbsum/7t37 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7t37 ProSAT]</span></td></tr>
</table>
</table>
== Function ==
== Function ==
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[[https://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>
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[https://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>
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<div style="background-color:#fffaf0;">
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== Publication Abstract from PubMed ==
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Transient receptor potential vanilloid 2 (TRPV2) is involved in many critical physiological and pathophysiological processes, making it a promising drug target. Here we present cryo-electron microscopy (cryo-EM) structures of rat TRPV2 in lipid nanodiscs activated by 2-aminoethoxydiphenyl borate (2-APB) and propose a TRPV2-specific 2-ABP binding site at the interface of S5 of one monomer and the S4-S5 linker of the adjacent monomer. In silico docking and electrophysiological studies confirm the key role of His521 and Arg539 in 2-APB activation of TRPV2. Additionally, electrophysiological experiments show that the combination of 2-APB and cannabidiol has a synergetic effect on TRPV2 activation, and cryo-EM structures demonstrate that both drugs were able to bind simultaneously. Together, our cryo-EM structures represent multiple functional states of the channel, providing a native picture of TRPV2 activation by small molecules and a structural framework for the development of TRPV2-specific activators.
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Structural insights into TRPV2 activation by small molecules.,Pumroy RA, Protopopova AD, Fricke TC, Lange IU, Haug FM, Nguyen PT, Gallo PN, Sousa BB, Bernardes GJL, Yarov-Yarovoy V, Leffler A, Moiseenkova-Bell VY Nat Commun. 2022 Apr 28;13(1):2334. doi: 10.1038/s41467-022-30083-3. PMID:35484159<ref>PMID:35484159</ref>
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==See Also==
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*[[Ion channels 3D structures|Ion channels 3D structures]]
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From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
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</div>
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<div class="pdbe-citations 7t37" style="background-color:#fffaf0;"></div>
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== References ==
== References ==
<references/>
<references/>
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</StructureSection>
</StructureSection>
[[Category: Large Structures]]
[[Category: Large Structures]]
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[[Category: Gallo, P N]]
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[[Category: Rattus norvegicus]]
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[[Category: Moiseenkova-Bell, V Y]]
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[[Category: Gallo PN]]
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[[Category: Protopopova, A D]]
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[[Category: Moiseenkova-Bell VY]]
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[[Category: Pumroy, R A]]
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[[Category: Protopopova AD]]
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[[Category: Ion channel]]
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[[Category: Pumroy RA]]
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[[Category: Transport protein]]
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[[Category: Trp channel]]
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[[Category: Trpv]]
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Current revision

Activated state of 2-APB and CBD-bound wildtype rat TRPV2 in nanodiscs

PDB ID 7t37

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