5c6p
From Proteopedia
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- | '''Unreleased structure''' | ||
- | + | ==protein C== | |
+ | <StructureSection load='5c6p' size='340' side='right' caption='[[5c6p]], [[Resolution|resolution]] 3.00Å' scene=''> | ||
+ | == Structural highlights == | ||
+ | <table><tr><td colspan='2'>[[5c6p]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5C6P OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5C6P FirstGlance]. <br> | ||
+ | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=4YH:(2S)-2-(3,4-DIMETHOXYPHENYL)-5-{[2-(3,4-DIMETHOXYPHENYL)ETHYL](METHYL)AMINO}-2-(PROPAN-2-YL)PENTANENITRILE'>4YH</scene></td></tr> | ||
+ | <tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[5c6o|5c6o]], [[5c6n|5c6n]]</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=5c6p FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5c6p OCA], [http://pdbe.org/5c6p PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5c6p RCSB], [http://www.ebi.ac.uk/pdbsum/5c6p PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5c6p ProSAT]</span></td></tr> | ||
+ | </table> | ||
+ | <div style="background-color:#fffaf0;"> | ||
+ | == Publication Abstract from PubMed == | ||
+ | Multidrug and toxic compound extrusion (MATE) transporters underpin multidrug resistance by using the H(+) or Na(+) electrochemical gradient to extrude different drugs across cell membranes. MATE transporters can be further parsed into the DinF, NorM and eukaryotic subfamilies based on their amino-acid sequence similarity. Here we report the 3.0 A resolution X-ray structures of a protonation-mimetic mutant of an H(+)-coupled DinF transporter, as well as of an H(+)-coupled DinF and a Na(+)-coupled NorM transporters in complexes with verapamil, a small-molecule pharmaceutical that inhibits MATE-mediated multidrug extrusion. Combining structure-inspired mutational and functional studies, we confirm the biological relevance of our crystal structures, reveal the mechanistic differences among MATE transporters, and suggest how verapamil inhibits MATE-mediated multidrug efflux. Our findings offer insights into how MATE transporters extrude chemically and structurally dissimilar drugs and could inform the design of new strategies for tackling multidrug resistance. | ||
- | + | Structural basis for the blockade of MATE multidrug efflux pumps.,Radchenko M, Symersky J, Nie R, Lu M Nat Commun. 2015 Aug 6;6:7995. doi: 10.1038/ncomms8995. PMID:26246409<ref>PMID:26246409</ref> | |
- | + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |
- | + | </div> | |
+ | <div class="pdbe-citations 5c6p" style="background-color:#fffaf0;"></div> | ||
+ | == References == | ||
+ | <references/> | ||
+ | __TOC__ | ||
+ | </StructureSection> | ||
[[Category: Lu, M]] | [[Category: Lu, M]] | ||
+ | [[Category: Protein]] | ||
+ | [[Category: Transport protein]] |
Revision as of 04:24, 21 September 2017
protein C
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