jm0c00780_si_001.pdf (4.81 MB)
Structure–Activity Relationships of Daptomycin Lipopeptides
journal contribution
posted on 2020-08-06, 11:43 authored by John A. Karas, Glen P. Carter, Benjamin P. Howden, Adrianna M. Turner, Olivia K. A. Paulin, James D. Swarbrick, Mark. A. Baker, Jian Li, Tony VelkovDaptomycin is a calcium-dependent
cyclic lipodepsipeptide derived
from the soil saprotroph Streptomyces roseosporus, and its antibiotic properties make it a key agent for treatment
of drug-resistant Gram-positive infections. It is most commonly used
clinically for the treatment of Gram-positive skin and skin structure
infections (SSSI), Staphylococcus aureus bacteremia,
and right-sided endocarditis infections associated with S.
aureus, including methicillin resistant S. aureus (MRSA). It has also been used “off-label” for Enterococcal
infections. There has been a tremendous amount of research investigating
its mode of action, resistance mechanisms, and biosynthesis of this
clinically important antimicrobial agent. Although we cover the latter
aspects in detail, the primary focus of this review is to provide
the most comprehensive and up-to-date reference for the medicinal
chemist on the structure–activity–toxicity of this important
class of lipopeptide antibiotics.
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antibiotic propertiesdrug-resistant Gram-positive infectionscalcium-dependent cyclic lipodepsip...resistance mechanismsMRSADaptomycin Lipopeptides DaptomycinGram-positive skinlatter aspectslipopeptide antibioticsSSSIaureusantimicrobial agentEnterococcal infectionssoil saprotroph Streptomyces roseos...right-sided endocarditis infectionsskin structure infections
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