7n0n: Difference between revisions

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 ==Activated state of 2-APB-bound wildtype rat TRPV2 in nanodiscs==
-<StructureSection load='7n0n' size='340' side='right'caption='[[7n0n]]' scene=''>
+<StructureSection load='7n0n' size='340' side='right'caption='[[7n0n]], [[Resolution|resolution]] 4.15&Aring;' scene=''>
 == Structural highlights ==
-<table><tr><td colspan='2'>Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=7N0N OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=7N0N FirstGlance]. <br>
+<table><tr><td colspan='2'>[[7n0n]] 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=7N0N OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=7N0N 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=7n0n FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7n0n OCA], [https://pdbe.org/7n0n PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7n0n RCSB], [https://www.ebi.ac.uk/pdbsum/7n0n PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7n0n ProSAT]</span></td></tr>
 </table>
+== Function ==
+[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>
+<div style="background-color:#fffaf0;">
+== Publication Abstract from PubMed ==
+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.
+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>
+From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
+</div>
+<div class="pdbe-citations 7n0n" style="background-color:#fffaf0;"></div>
+== References ==
+<references/>
 __TOC__
 </StructureSection>
 [[Category: Large Structures]]
+[[Category: Rattus norvegicus]]
 [[Category: Gallo PN]]
 [[Category: Moiseenkova-Bell VY]]
 [[Category: Protopopova AD]]
 [[Category: Pumroy RA]]