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dc.contributor.authorTaylor, Scott D.
dc.contributor.authorPalmer, Michael 17:59:05 (GMT) 17:59:05 (GMT)
dc.descriptionThe final publication is available at Elsevier via © 2016.en
dc.description.abstractDaptomycin is a lipopeptide antibiotic produced by the soil bacterium Streptomyces roseosporus that is clinically used to treat severe infections with Gram-positive bacteria. In this review, we discuss the mode of action of this important antibiotic. Although daptomycin is structurally related to amphomycin and similar lipopeptides that inhibit peptidoglycan biosynthesis, experimental studies have not produced clear evidence that daptomycin shares their action mechanism. Instead, the best characterized effect of daptomycin is the permeabilization and depolarization of the bacterial cell membrane. This activity, which can account for daptomycin's bactericidal effect, correlates with the level of phosphatidylglycerol (PG) in the membrane. Accordingly, reduced synthesis of PG or its increased conversion to lysyl-PG promotes bacterial resistance to daptomycin. While other resistance mechanisms suggest that daptomycin may indeed directly interfere with cell wall synthesis or cell division, such effects still await direct experimental confirmation. Daptomycin's complex structure and biosynthesis have hampered the analysis of its structure activity relationships. Novel methods of total synthesis, including a recent one that is carried out entirely on a solid phase, will enable a more thorough and systematic exploration of the sequence space.en
dc.subjectBacterial membranesen
dc.subjectCalcium-dependent lipopeptide antibioticsen
dc.subjectCationic antimicrobial peptidesen
dc.subjectCell-wall biosynthesisen
dc.subjectDependent antibiotic daptomycinen
dc.subjectGram-positive infectionsen
dc.subjectLipopeptide antibioticsen
dc.subjectMembrane potentialen
dc.subjectPeptidoglycan synthesisen
dc.subjectPulmonary surfactanten
dc.subjectResistant staphylococcus-aureusen
dc.titleThe action mechanism of daptomycinen
dcterms.bibliographicCitationTaylor, S. D., & Palmer, M. (2016). The action mechanism of daptomycin. Bioorganic & Medicinal Chemistry, 24(24), 6253–6268.
uws.contributor.affiliation1Faculty of Scienceen

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