1t5m

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{{Seed}}
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{{STRUCTURE_1t5m| PDB=1t5m | SCENE= }}
{{STRUCTURE_1t5m| PDB=1t5m | SCENE= }}
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'''Structural transitions as determinants of the action of the calcium-dependent antibiotic daptomycin'''
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===Structural transitions as determinants of the action of the calcium-dependent antibiotic daptomycin===
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==Overview==
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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.
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(as it appears on PubMed at http://www.pubmed.gov), where 15271353 is the PubMed ID number.
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{{ABSTRACT_PUBMED_15271353}}
==About this Structure==
==About this Structure==
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Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1T5M OCA].
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Full experimental information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1T5M OCA].
==Reference==
==Reference==
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[[Category: Daptomycin]]
[[Category: Daptomycin]]
[[Category: Drug]]
[[Category: Drug]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 09:33:19 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jul 29 08:55:21 2008''

Revision as of 05:55, 29 July 2008

Image:1t5m.png

Template:STRUCTURE 1t5m

Structural transitions as determinants of the action of the calcium-dependent antibiotic daptomycin

Template:ABSTRACT PUBMED 15271353

About this Structure

Full experimental 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 Tue Jul 29 08:55:21 2008

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