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==Structural Insights into the Anti- Methicillin-Resistant Staphylococcus aureus (MRSA) Activity of Ceftobiprole== | ==Structural Insights into the Anti- Methicillin-Resistant Staphylococcus aureus (MRSA) Activity of Ceftobiprole== | ||
<StructureSection load='4dki' size='340' side='right' caption='[[4dki]], [[Resolution|resolution]] 2.90Å' scene=''> | <StructureSection load='4dki' size='340' side='right' caption='[[4dki]], [[Resolution|resolution]] 2.90Å' scene=''> | ||
== Structural highlights == | == Structural highlights == | ||
<table><tr><td colspan='2'>[[4dki]] is a 2 chain structure with sequence from [http://en.wikipedia.org/wiki/ | <table><tr><td colspan='2'>[[4dki]] is a 2 chain structure with sequence from [http://en.wikipedia.org/wiki/Staac Staac]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4DKI OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4DKI FirstGlance]. <br> | ||
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=BCT:BICARBONATE+ION'>BCT</scene>, <scene name='pdbligand=CD:CADMIUM+ION'>CD</scene>, <scene name='pdbligand=CL:CHLORIDE+ION'>CL</scene>, <scene name='pdbligand=RB6:(2R)-2-[(1R)-1-{[(2Z)-2-(5-AMINO-1,2,4-THIADIAZOL-3-YL)-2-(HYDROXYIMINO)ACETYL]AMINO}-2-OXOETHYL]-5-({2-OXO-1-[(3R)-PYRROLIDIN-3-YL]-2,5-DIHYDRO-1H-PYRROL-3-YL}METHYL)-3,6-DIHYDRO-2H-1,3-THIAZINE-4-CARBOXYLIC+ACID'>RB6</scene></td></tr> | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=BCT:BICARBONATE+ION'>BCT</scene>, <scene name='pdbligand=CD:CADMIUM+ION'>CD</scene>, <scene name='pdbligand=CL:CHLORIDE+ION'>CL</scene>, <scene name='pdbligand=RB6:(2R)-2-[(1R)-1-{[(2Z)-2-(5-AMINO-1,2,4-THIADIAZOL-3-YL)-2-(HYDROXYIMINO)ACETYL]AMINO}-2-OXOETHYL]-5-({2-OXO-1-[(3R)-PYRROLIDIN-3-YL]-2,5-DIHYDRO-1H-PYRROL-3-YL}METHYL)-3,6-DIHYDRO-2H-1,3-THIAZINE-4-CARBOXYLIC+ACID'>RB6</scene></td></tr> | ||
<tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">mecA, SACOL0033 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id= | <tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">mecA, SACOL0033 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=93062 STAAC])</td></tr> | ||
<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Serine-type_D-Ala-D-Ala_carboxypeptidase Serine-type D-Ala-D-Ala carboxypeptidase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.16.4 3.4.16.4] </span></td></tr> | <tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Serine-type_D-Ala-D-Ala_carboxypeptidase Serine-type D-Ala-D-Ala carboxypeptidase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.16.4 3.4.16.4] </span></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=4dki FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4dki OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4dki RCSB], [http://www.ebi.ac.uk/pdbsum/4dki PDBsum]</span></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=4dki FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4dki OCA], [http://pdbe.org/4dki PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=4dki RCSB], [http://www.ebi.ac.uk/pdbsum/4dki PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=4dki ProSAT]</span></td></tr> | ||
</table> | </table> | ||
<div style="background-color:#fffaf0;"> | <div style="background-color:#fffaf0;"> | ||
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From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | ||
</div> | </div> | ||
<div class="pdbe-citations 4dki" style="background-color:#fffaf0;"></div> | |||
==See Also== | ==See Also== | ||
| Line 24: | Line 26: | ||
</StructureSection> | </StructureSection> | ||
[[Category: Serine-type D-Ala-D-Ala carboxypeptidase]] | [[Category: Serine-type D-Ala-D-Ala carboxypeptidase]] | ||
[[Category: | [[Category: Staac]] | ||
[[Category: Gretes, M C]] | [[Category: Gretes, M C]] | ||
[[Category: Lovering, A L]] | [[Category: Lovering, A L]] | ||
Revision as of 16:48, 11 August 2016
Structural Insights into the Anti- Methicillin-Resistant Staphylococcus aureus (MRSA) Activity of CeftobiproleStructural Insights into the Anti- Methicillin-Resistant Staphylococcus aureus (MRSA) Activity of Ceftobiprole
Structural highlights
Publication Abstract from PubMedMethicillin-resistant Staphylococcus aureus (MRSA) is an antibiotic resistant strain of Staphylococcus aureus afflicting hospitals and communities worldwide. Of greatest concern is its development of resistance to current last-line-of-defense antibiotics; new therapeutics are urgently needed to combat this pathogen. Ceftobiprole is a recently developed, latest-generation cephalosporin, and has been the first to show activity against MRSA by inhibiting essential peptidoglycan transpeptidases, including the beta-lactam resistance determinant PBP2a, from MRSA. Here we present the structure of the complex of ceftobiprole bound to PBP2a. This structure provides the first look at the molecular details of an effective beta-lactam:resistant PBP interaction, leading to new insights into the mechanism of ceftobiprole efficacy against MRSA. Structural Insights into the Anti- Methicillin-Resistant Staphylococcus aureus (MRSA) Activity of Ceftobiprole.,Lovering AL, Gretes MC, Safadi SS, Danel F, De Castro L, Page MG, Strynadka NC J Biol Chem. 2012 Jul 19. PMID:22815485[1] From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. See AlsoReferences
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