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- W2185184588 abstract "Daptomycin is a Ca(+2)-dependent cyclic lipodepsipeptide antibiotic used clinically to treat serious infections caused by Gram-positive bacteria. The recent appearance of daptomycin-resistant strains, daptomycin's lack of activity in the presence of lung surfactant, and its incompletely understood mechanism of action underscores the need for establishing detailed structure-activity relationships. Here we report a solid-phase synthesis of a daptomycin analog in which Thr4, 3-MeGlu12 and Kyn13 in daptomycin were replaced with Ser, Glu and Trp residues, respectively (Dap-S4-E12-W13). The Thr4 to Ser4 substitution was detrimental to activity, as Dap-S4-E12-W13 was at least 20-fold less active at physiological Ca(+2) concentration than Dap-E12-W13. Much of its activity could be recovered at high (100 mM) Ca(+2) concentration, suggesting that the residue at position 4 affects Ca(+2) binding and, consequently, biological activity." @default.
- W2185184588 created "2016-06-24" @default.
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- W2185184588 date "2015-12-01" @default.
- W2185184588 modified "2023-10-18" @default.
- W2185184588 title "Solid-phase synthesis and in vitro biological activity of a Thr4→Ser4 analog of daptomycin" @default.
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- W2185184588 doi "https://doi.org/10.1016/j.bmcl.2015.10.072" @default.
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