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1t5m
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| - | [[Image:1t5m.gif|left|200px]]<br /><applet load="1t5m" size="350" color="white" frame="true" align="right" spinBox="true" | ||
| - | caption="1t5m" /> | ||
| - | '''Structural transitions as determinants of the action of the calcium-dependent antibiotic daptomycin'''<br /> | ||
| - | == | + | ==Structural transitions as determinants of the action of the calcium-dependent antibiotic daptomycin== |
| + | <StructureSection load='1t5m' size='340' side='right'caption='[[1t5m]]' scene=''> | ||
| + | == Structural highlights == | ||
| + | <table><tr><td colspan='2'>[[1t5m]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/Streptomyces_filamentosus Streptomyces filamentosus]. Full experimental information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1T5M OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=1T5M FirstGlance]. <br> | ||
| + | </td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">Solution NMR</td></tr> | ||
| + | <tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=DAL:D-ALANINE'>DAL</scene>, <scene name='pdbligand=DKA:DECANOIC+ACID'>DKA</scene>, <scene name='pdbligand=DSG:D-ASPARAGINE'>DSG</scene>, <scene name='pdbligand=DSN:D-SERINE'>DSN</scene>, <scene name='pdbligand=KYN:(2S)-2-AMINO-4-(2-AMINOPHENYL)-4-OXOBUTANOIC+ACID'>KYN</scene>, <scene name='pdbligand=LME:(2S,3R)-2-AZANYL-3-METHYL-PENTANEDIOIC+ACID'>LME</scene>, <scene name='pdbligand=ORN:L-ORNITHINE'>ORN</scene>, <scene name='pdbligand=PRD_000217:Daptomycin'>PRD_000217</scene></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=1t5m FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1t5m OCA], [https://pdbe.org/1t5m PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=1t5m RCSB], [https://www.ebi.ac.uk/pdbsum/1t5m PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=1t5m ProSAT]</span></td></tr> | ||
| + | </table> | ||
| + | <div style="background-color:#fffaf0;"> | ||
| + | == Publication Abstract from PubMed == | ||
Daptomycin is a cyclic anionic lipopeptide antibiotic recently approved for the treatment of complicated skin infections (Cubicin). Its function is dependent on calcium (as Ca2+). Circular dichroism spectroscopy indicated that daptomycin experienced two structural transitions: a transition upon interaction of daptomycin with Ca2+, and a further transition upon interaction with Ca2+ and the bacterial acidic phospholipid, phosphatidyl glycerol. The Ca2+-dependent insertion of daptomycin into model membranes promoted mild and more pronounced perturbations as assessed by the increase of lipid flip-flop and membrane leakage, respectively. The NMR structure of daptomycin indicated that Ca2+ induced a conformational change in daptomycin that increased its amphipathicity. These results are consistent with the hypothesis that the association of Ca2+ with daptomycin permits it to interact with bacterial membranes with effects that are similar to those of the cationic antimicrobial peptides. | Daptomycin is a cyclic anionic lipopeptide antibiotic recently approved for the treatment of complicated skin infections (Cubicin). Its function is dependent on calcium (as Ca2+). Circular dichroism spectroscopy indicated that daptomycin experienced two structural transitions: a transition upon interaction of daptomycin with Ca2+, and a further transition upon interaction with Ca2+ and the bacterial acidic phospholipid, phosphatidyl glycerol. The Ca2+-dependent insertion of daptomycin into model membranes promoted mild and more pronounced perturbations as assessed by the increase of lipid flip-flop and membrane leakage, respectively. The NMR structure of daptomycin indicated that Ca2+ induced a conformational change in daptomycin that increased its amphipathicity. These results are consistent with the hypothesis that the association of Ca2+ with daptomycin permits it to interact with bacterial membranes with effects that are similar to those of the cationic antimicrobial peptides. | ||
| - | + | Structural transitions as determinants of the action of the calcium-dependent antibiotic daptomycin.,Jung D, Rozek A, Okon M, Hancock RE Chem Biol. 2004 Jul;11(7):949-57. PMID:15271353<ref>PMID:15271353</ref> | |
| - | + | ||
| - | + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |
| - | + | </div> | |
| - | + | <div class="pdbe-citations 1t5m" style="background-color:#fffaf0;"></div> | |
| - | + | == References == | |
| - | + | <references/> | |
| - | + | __TOC__ | |
| - | + | </StructureSection> | |
| - | [[Category: | + | [[Category: Large Structures]] |
| - | [[Category: | + | [[Category: Streptomyces filamentosus]] |
| - | [[Category: | + | [[Category: Hancock RE]] |
| - | [[Category: | + | [[Category: Jung D]] |
| - | [[Category: | + | [[Category: Okon M]] |
| - | [[Category: | + | [[Category: Rozek A]] |
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Current revision
Structural transitions as determinants of the action of the calcium-dependent antibiotic daptomycin
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