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6b5v

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==Structure of TRPV5 in complex with econazole==
==Structure of TRPV5 in complex with econazole==
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<StructureSection load='6b5v' size='340' side='right'caption='[[6b5v]], [[Resolution|resolution]] 4.80&Aring;' scene=''>
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<SX load='6b5v' size='340' side='right' viewer='molstar' caption='[[6b5v]], [[Resolution|resolution]] 4.80&Aring;' scene=''>
== Structural highlights ==
== Structural highlights ==
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<table><tr><td colspan='2'>[[6b5v]] is a 4 chain structure with sequence from [http://en.wikipedia.org/wiki/European_rabbit European rabbit]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6B5V OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6B5V FirstGlance]. <br>
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<table><tr><td colspan='2'>[[6b5v]] is a 4 chain structure with sequence from [https://en.wikipedia.org/wiki/Oryctolagus_cuniculus Oryctolagus cuniculus]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6B5V OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=6B5V FirstGlance]. <br>
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</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=CA:CALCIUM+ION'>CA</scene>, <scene name='pdbligand=ECL:1-[(2R)-2-[(4-CHLOROBENZYL)OXY]-2-(2,4-DICHLOROPHENYL)ETHYL]-1H-IMIDAZOLE'>ECL</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]] 4.8&#8491;</td></tr>
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<tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">Trpv5, Ecac1 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9986 European rabbit])</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=CA:CALCIUM+ION'>CA</scene>, <scene name='pdbligand=ECL:1-[(2R)-2-[(4-CHLOROBENZYL)OXY]-2-(2,4-DICHLOROPHENYL)ETHYL]-1H-IMIDAZOLE'>ECL</scene></td></tr>
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<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=6b5v FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6b5v OCA], [http://pdbe.org/6b5v PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6b5v RCSB], [http://www.ebi.ac.uk/pdbsum/6b5v PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6b5v ProSAT]</span></td></tr>
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<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=6b5v FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6b5v OCA], [https://pdbe.org/6b5v PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=6b5v RCSB], [https://www.ebi.ac.uk/pdbsum/6b5v PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=6b5v ProSAT]</span></td></tr>
</table>
</table>
== Function ==
== Function ==
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[[http://www.uniprot.org/uniprot/TRPV5_RABIT TRPV5_RABIT]] Constitutively active calcium selective cation channel thought to be involved in Ca(2+) reabsorption in kidney and intestine (PubMed:12574114). Required for normal Ca(2+) reabsorption in the kidney distal convoluted tubules (By similarity). The channel is activated by low internal calcium level and the current exhibits an inward rectification (By similarity). A Ca(2+)-dependent feedback regulation includes fast channel inactivation and slow current decay (By similarity). Heteromeric assembly with TRPV6 seems to modify channel properties. TRPV5-TRPV6 heteromultimeric concatemers exhibit voltage-dependent gating (PubMed:12574114).[UniProtKB:P69744][UniProtKB:Q9NQA5]<ref>PMID:10085067</ref> <ref>PMID:11035011</ref> <ref>PMID:12574114</ref>
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[https://www.uniprot.org/uniprot/TRPV5_RABIT TRPV5_RABIT] Constitutively active calcium selective cation channel thought to be involved in Ca(2+) reabsorption in kidney and intestine (PubMed:12574114). Required for normal Ca(2+) reabsorption in the kidney distal convoluted tubules (By similarity). The channel is activated by low internal calcium level and the current exhibits an inward rectification (By similarity). A Ca(2+)-dependent feedback regulation includes fast channel inactivation and slow current decay (By similarity). Heteromeric assembly with TRPV6 seems to modify channel properties. TRPV5-TRPV6 heteromultimeric concatemers exhibit voltage-dependent gating (PubMed:12574114).[UniProtKB:P69744][UniProtKB:Q9NQA5]<ref>PMID:10085067</ref> <ref>PMID:11035011</ref> <ref>PMID:12574114</ref>
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<div style="background-color:#fffaf0;">
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== Publication Abstract from PubMed ==
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The transient receptor potential vanilloid 5 (TRPV5) channel is a member of the transient receptor potential (TRP) channel family, which is highly selective for Ca(2+), that is present primarily at the apical membrane of distal tubule epithelial cells in the kidney and plays a key role in Ca(2+) reabsorption. Here we present the structure of the full-length rabbit TRPV5 channel as determined using cryo-EM in complex with its inhibitor econazole. This structure reveals that econazole resides in a hydrophobic pocket analogous to that occupied by phosphatidylinositides and vanilloids in TRPV1, thus suggesting conserved mechanisms for ligand recognition and lipid binding among TRPV channels. The econazole-bound TRPV5 structure adopts a closed conformation with a distinct lower gate that occludes Ca(2+) permeation through the channel. Structural comparisons between TRPV5 and other TRPV channels, complemented with molecular dynamics (MD) simulations of the econazole-bound TRPV5 structure, allowed us to gain mechanistic insight into TRPV5 channel inhibition by small molecules.
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Structural basis of TRPV5 channel inhibition by econazole revealed by cryo-EM.,Hughes TET, Lodowski DT, Huynh KW, Yazici A, Del Rosario J, Kapoor A, Basak S, Samanta A, Han X, Chakrapani S, Zhou ZH, Filizola M, Rohacs T, Han S, Moiseenkova-Bell VY Nat Struct Mol Biol. 2018 Jan;25(1):53-60. doi: 10.1038/s41594-017-0009-1. Epub, 2018 Jan 1. PMID:29323279<ref>PMID:29323279</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 6b5v" style="background-color:#fffaf0;"></div>
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== References ==
== References ==
<references/>
<references/>
__TOC__
__TOC__
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</StructureSection>
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</SX>
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[[Category: European rabbit]]
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[[Category: Large Structures]]
[[Category: Large Structures]]
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[[Category: Basak, S]]
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[[Category: Oryctolagus cuniculus]]
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[[Category: Chakrapani, S]]
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[[Category: Basak S]]
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[[Category: Filizola, M]]
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[[Category: Chakrapani S]]
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[[Category: Han, S]]
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[[Category: Filizola M]]
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[[Category: Hughes, T E.T]]
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[[Category: Han S]]
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[[Category: Huynh, K W]]
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[[Category: Hughes TET]]
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[[Category: Kapoor, A]]
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[[Category: Huynh KW]]
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[[Category: Lodowski, D T]]
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[[Category: Kapoor A]]
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[[Category: Moiseenkova-Bell, V Y]]
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[[Category: Lodowski DT]]
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[[Category: Rohacs, T]]
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[[Category: Moiseenkova-Bell VY]]
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[[Category: Rosario, J del]]
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[[Category: Rohacs T]]
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[[Category: Samanta, A]]
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[[Category: Samanta A]]
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[[Category: Yazici, A]]
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[[Category: Yazici A]]
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[[Category: Zhou, Z H]]
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[[Category: Zhou ZH]]
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[[Category: Cryo-em]]
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[[Category: Del Rosario J]]
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[[Category: Econazole]]
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[[Category: Membrane protein]]
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[[Category: Transient receptor potential channel]]
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[[Category: Trpv5]]
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Current revision

Structure of TRPV5 in complex with econazole

6b5v, resolution 4.80Å

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