1t5m

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|PDB= 1t5m |SIZE=350|CAPTION= <scene name='initialview01'>1t5m</scene>
|PDB= 1t5m |SIZE=350|CAPTION= <scene name='initialview01'>1t5m</scene>
|SITE=
|SITE=
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|LIGAND= <scene name='pdbligand=DKA:DECANOIC ACID'>DKA</scene>
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|LIGAND= <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:KYNURENINE'>KYN</scene>, <scene name='pdbligand=MEG:(2S,3R)-3-METHYL-GLUTAMIC+ACID'>MEG</scene>, <scene name='pdbligand=ORN:ORNITHINE'>ORN</scene>
|ACTIVITY=
|ACTIVITY=
|GENE=
|GENE=
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|DOMAIN=
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|RELATEDENTRY=[[1t5n|1T5N]]
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1t5m FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1t5m OCA], [http://www.ebi.ac.uk/pdbsum/1t5m PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1t5m RCSB]</span>
}}
}}
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[[Category: Okon, M.]]
[[Category: Okon, M.]]
[[Category: Rozek, A.]]
[[Category: Rozek, A.]]
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[[Category: DKA]]
 
[[Category: antibiotic]]
[[Category: antibiotic]]
[[Category: calcium-dependent]]
[[Category: calcium-dependent]]
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[[Category: drug]]
[[Category: drug]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Mar 20 14:14:06 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Mar 30 23:51:36 2008''

Revision as of 20:51, 30 March 2008


PDB ID 1t5m

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Ligands: , , , , , ,
Related: 1T5N


Resources: FirstGlance, OCA, PDBsum, RCSB
Coordinates: save as pdb, mmCIF, xml



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]. 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

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