"CLipP"ing on lipids to generate antibacterial lipopeptides

Chem Sci. 2020 May 20;11(22):5759-5765. doi: 10.1039/d0sc01814g.


We herein report the synthesis and biological and computational evaluation of 12 linear analogues of the cyclic lipopeptide battacin, enabled by Cysteine Lipidation on a Peptide or Amino Acid (CLipPA) technology. Several of the novel "CLipP"ed lipopeptides exhibited low micromolar MICs and MBCs against both Gram-negative and Gram-positive bacteria. The mechanism of action was then simulated with the MIC data using computational methods.