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| | <StructureSection load='5c6o' size='340' side='right'caption='[[5c6o]], [[Resolution|resolution]] 3.00Å' scene=''> | | <StructureSection load='5c6o' size='340' side='right'caption='[[5c6o]], [[Resolution|resolution]] 3.00Å' scene=''> |
| | == Structural highlights == | | == Structural highlights == |
| - | <table><tr><td colspan='2'>[[5c6o]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/Bachd Bachd]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5C6O OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5C6O FirstGlance]. <br> | + | <table><tr><td colspan='2'>[[5c6o]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/Alkalihalobacillus_halodurans_C-125 Alkalihalobacillus halodurans C-125]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5C6O OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=5C6O 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> | + | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><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">[[5c6p|5c6p]], [[5c6n|5c6n]]</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=5c6o FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5c6o OCA], [https://pdbe.org/5c6o PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=5c6o RCSB], [https://www.ebi.ac.uk/pdbsum/5c6o PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=5c6o ProSAT]</span></td></tr> |
| - | <tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">BH2163 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=272558 BACHD])</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=5c6o FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5c6o OCA], [http://pdbe.org/5c6o PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5c6o RCSB], [http://www.ebi.ac.uk/pdbsum/5c6o PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5c6o ProSAT]</span></td></tr> | + | |
| | </table> | | </table> |
| | + | == Function == |
| | + | [https://www.uniprot.org/uniprot/Q9KAX3_HALH5 Q9KAX3_HALH5] |
| | <div style="background-color:#fffaf0;"> | | <div style="background-color:#fffaf0;"> |
| | == Publication Abstract from PubMed == | | == Publication Abstract from PubMed == |
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| | __TOC__ | | __TOC__ |
| | </StructureSection> | | </StructureSection> |
| - | [[Category: Bachd]] | + | [[Category: Alkalihalobacillus halodurans C-125]] |
| | [[Category: Large Structures]] | | [[Category: Large Structures]] |
| - | [[Category: Lu, M]] | + | [[Category: Lu M]] |
| - | [[Category: Protein binding]]
| + | |
| - | [[Category: Transport protein]]
| + | |
| Structural highlights
Function
Q9KAX3_HALH5
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[1]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
References
- ↑ Radchenko M, Symersky J, Nie R, Lu M. Structural basis for the blockade of MATE multidrug efflux pumps. Nat Commun. 2015 Aug 6;6:7995. doi: 10.1038/ncomms8995. PMID:26246409 doi:http://dx.doi.org/10.1038/ncomms8995
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