Journal article

Structure-Activity Relationships of Daptomycin Lipopeptides

John A Karas, Glen P Carter, Benjamin P Howden, Adrianna M Turner, Olivia KA Paulin, James D Swarbrick, Mark A Baker, Jian Li, Tony Velkov

Journal of Medicinal Chemistry | AMER CHEMICAL SOC | Published : 2020


Daptomycin 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 importa..

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Funding Acknowledgements

T.V and J.L. are supported by research grants from the National Institute of Allergy and Infectious Diseases (NIAID) of the National Institutes of Health (NIH) and Australian National Health and Medical Research Council (NHMRC). J.L. is an NHMRC Principal Research Fellow. B.P.H. and G.P.C. are also supported byNHMRCresearch grants. The content is solely the responsibility of the authors and does not necessarily represent the official views of the NIAID or the NIH.