1t5m
From Proteopedia
(New page: 200px<br /><applet load="1t5m" size="450" color="white" frame="true" align="right" spinBox="true" caption="1t5m" /> '''Structural transitions as determinants of th...) |
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| - | [[Image:1t5m.gif|left|200px]]<br /><applet load="1t5m" size=" | + | [[Image:1t5m.gif|left|200px]]<br /><applet load="1t5m" size="350" color="white" frame="true" align="right" spinBox="true" |
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'''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'''<br /> | ||
==Overview== | ==Overview== | ||
| - | Daptomycin is a cyclic anionic lipopeptide antibiotic recently approved | + | 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. |
==About this Structure== | ==About this Structure== | ||
| - | 1T5M is a [http://en.wikipedia.org/wiki/Protein_complex Protein complex] structure of sequences from [http://en.wikipedia.org/wiki/ ] with DKA as [http://en.wikipedia.org/wiki/ligand ligand]. Full crystallographic information is available from [http:// | + | 1T5M is a [http://en.wikipedia.org/wiki/Protein_complex Protein complex] structure of sequences from [http://en.wikipedia.org/wiki/ ] with <scene name='pdbligand=DKA:'>DKA</scene> as [http://en.wikipedia.org/wiki/ligand ligand]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1T5M OCA]. |
==Reference== | ==Reference== | ||
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:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=15271353 15271353] | 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:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=15271353 15271353] | ||
[[Category: Protein complex]] | [[Category: Protein complex]] | ||
| - | [[Category: Hancock, R | + | [[Category: Hancock, R E.]] |
[[Category: Jung, D.]] | [[Category: Jung, D.]] | ||
[[Category: Okon, M.]] | [[Category: Okon, M.]] | ||
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[[Category: drug]] | [[Category: drug]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 15:10:07 2008'' |
Revision as of 13:10, 21 February 2008
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Structural transitions as determinants of the action of the calcium-dependent antibiotic daptomycin
Overview
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.
About this Structure
1T5M is a Protein complex structure of sequences from [1] with as ligand. Full crystallographic information is available from OCA.
Reference
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
Page seeded by OCA on Thu Feb 21 15:10:07 2008
Categories: Protein complex | Hancock, R E. | Jung, D. | Okon, M. | Rozek, A. | DKA | Antibiotic | Calcium-dependent | Cubicin | Cyclic lipopeptide | Daptomycin | Drug
