6juh
From Proteopedia
(Difference between revisions)
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- | '''Unreleased structure''' | ||
- | + | ==structure of CavAb in complex with efonidipine== | |
+ | <StructureSection load='6juh' size='340' side='right'caption='[[6juh]], [[Resolution|resolution]] 3.00Å' scene=''> | ||
+ | == Structural highlights == | ||
+ | <table><tr><td colspan='2'>[[6juh]] is a 4 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6JUH OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6JUH FirstGlance]. <br> | ||
+ | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=C9X:2-[phenyl-(phenylmethyl)amino]ethyl+(4~{R})-5-(5,5-dimethyl-2-oxidanylidene-1,3,2$l^{5}-dioxaphosphinan-2-yl)-2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3-carboxylate'>C9X</scene>, <scene name='pdbligand=CA:CALCIUM+ION'>CA</scene>, <scene name='pdbligand=G3P:SN-GLYCEROL-3-PHOSPHATE'>G3P</scene>, <scene name='pdbligand=MC3:1,2-DIMYRISTOYL-RAC-GLYCERO-3-PHOSPHOCHOLINE'>MC3</scene>, <scene name='pdbligand=PX4:1,2-DIMYRISTOYL-SN-GLYCERO-3-PHOSPHOCHOLINE'>PX4</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=6juh FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6juh OCA], [http://pdbe.org/6juh PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6juh RCSB], [http://www.ebi.ac.uk/pdbsum/6juh PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6juh ProSAT]</span></td></tr> | ||
+ | </table> | ||
+ | <div style="background-color:#fffaf0;"> | ||
+ | == Publication Abstract from PubMed == | ||
+ | Efonidipine is a dual L-/T- type calcium channel blocker with a slow onset of action and a long lasting effect that exibihits antihypertensive and nephroprotective effects. differs from most other DHPs which can induce reflex tachycardia. Efonidipine reduces blood pressure without decreasing cardiac output and exerts organ-protective effects on the heart and kidney. In order to investigate how efonidipine block voltage-gated Ca(2+) channel, we determined the crystal structure of CaVAb in complex with efonidipine at atomic resolution using x-ray crystallography. Our results reveal that efonidipine targets the central cavity of a model voltage-gated calcium channel underneath its selectivity filter and occlude the channel in an inactivated state. Binding of efonidipine does not break down the fourfold symmetry of the quaternary structure and its pore structure. Our work provides the structural basis for efonidipine block of a voltage-gated Ca(2+) channel at the molecular level. | ||
- | + | Structural basis for efonidipine block of a voltage-gated Ca(2+) channel.,Xu F, Xiong W, Huang Y, Shen J, Zhou D, Tang L Biochem Biophys Res Commun. 2019 Jun 4;513(3):631-634. doi:, 10.1016/j.bbrc.2019.03.176. Epub 2019 Apr 10. PMID:30981510<ref>PMID:30981510</ref> | |
- | + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |
- | [[Category: | + | </div> |
+ | <div class="pdbe-citations 6juh" style="background-color:#fffaf0;"></div> | ||
+ | == References == | ||
+ | <references/> | ||
+ | __TOC__ | ||
+ | </StructureSection> | ||
+ | [[Category: Large Structures]] | ||
+ | [[Category: Tang, L]] | ||
+ | [[Category: Xu, F]] | ||
+ | [[Category: Membrane protein]] | ||
+ | [[Category: Voltage-gated calcium channel block]] |
Revision as of 06:40, 6 November 2019
structure of CavAb in complex with efonidipine
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