An atomic perspective on improving daptomycin's activity

• Published in: Biochimica et biophysica acta. General subjects Vol. 1865; no. 8; p. 129918
• Main Authors: Blasco, Pilar, Zhang, Chunlei, Chow, Hoi Yee, Chen, Guanhua, Wu, Yongsheng, Li, Xuechen
• Format: Journal Article
• Language: English
• Published: Netherlands Elsevier B.V 01.08.2021
• Subjects: antibacterial properties; calcium; Calcium dependent antibiotics; Cyclic peptide; cytotoxicity; Daptomycin; Enterococcus; kynurenine; methicillin-resistant Staphylococcus aureus; methylation; molecular dynamics; Molecular dynamics (MD); Nuclear magnetic resonance (NMR); nuclear magnetic resonance spectroscopy; Oligomerization; pharmacokinetics; tryptophan; Molecular dynamics (MD); Cyclic peptide; Oligomerization; Calcium dependent antibiotics; Nuclear magnetic resonance (NMR); Daptomycin

Recently, through comprehensive medicinal chemistry efforts, we have found a new daptomycin analogue, termed kynomycin, showing enhanced activity against both methicillin-resistant S. aureus and vancomycin-resistant Enterococcus in vitro and in vivo, with improved pharmacokinetics and lower cytotoxi...