Structure-Activity Relationships of Daptomycin Lipopeptides.

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Karas JA, Carter GP, Howden BP, Turner AM, Paulin OKA, Swarbrick JD, Baker MA, Li J, Velkov T

Structure-Activity Relationships of Daptomycin Lipopeptides.

J Med Chem. 2020 Nov 25;63(22):13266-13290. doi: 10.1021/acs.jmedchem.0c00780. Epub 2020 Aug 6.

PubMed ID

32687352 [ View in PubMed

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Abstract

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 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.

DrugBank Data that Cites this Article

Drugs

Daptomycin

Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Daptomycin	Cytoplasmic membrane	Group	Bacteria	Yes	Incorporation into and destabilization	Details