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- W3106980446 abstract "Abstract Daptomycin (DAP) is a calcium (Ca 2+ )‐dependent FDA‐approved antibiotic drug for the treatment of Gram‐positive infections. It possesses a complex pharmacophore hampering derivatization and/or synthesis of analogues. To mimic the Ca 2+ ‐binding effect, we used a chemoenzymatic approach to modify the tryptophan (Trp) residue of DAP and synthesize kinetically characterized and structurally elucidated regiospecific Trp‐modified DAP analogues. We demonstrated that the modified DAPs are several times more active than the parent molecule against antibiotic‐susceptible and antibiotic‐resistant Gram‐positive bacteria. Strikingly, and in contrast to the parent molecule, the DAP derivatives do not rely on calcium or any additional elements for activity." @default.
- W3106980446 created "2020-12-07" @default.
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- W3106980446 date "2021-01-26" @default.
- W3106980446 modified "2023-10-14" @default.
- W3106980446 title "Regiospecific Synthesis of Calcium‐Independent Daptomycin Antibiotics using a Chemoenzymatic Method" @default.
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- W3106980446 doi "https://doi.org/10.1002/chem.202005100" @default.
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