1t5m: Difference between revisions
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'''Structural transitions as determinants of the action of the calcium-dependent antibiotic daptomycin''' | {{Structure | ||
|PDB= 1t5m |SIZE=350|CAPTION= <scene name='initialview01'>1t5m</scene> | |||
|SITE= | |||
|LIGAND= <scene name='pdbligand=DKA:DECANOIC ACID'>DKA</scene> | |||
|ACTIVITY= | |||
|GENE= | |||
}} | |||
'''Structural transitions as determinants of the action of the calcium-dependent antibiotic daptomycin''' | |||
==Overview== | ==Overview== | ||
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==About this Structure== | ==About this Structure== | ||
1T5M is a [ | 1T5M is a [[Protein complex]] structure of sequences from [http://en.wikipedia.org/wiki/ ]. 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:// | 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://www.ncbi.nlm.nih.gov/pubmed/15271353 15271353] | ||
[[Category: Protein complex]] | [[Category: Protein complex]] | ||
[[Category: Hancock, R E.]] | [[Category: Hancock, R E.]] | ||
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[[Category: drug]] | [[Category: drug]] | ||
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Mar 20 14:14:06 2008'' | ||
Revision as of 12:14, 20 March 2008
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| Ligands: | DKA | ||||||||||||
| 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
Page seeded by OCA on Thu Mar 20 14:14:06 2008
