Partial [alphaMe]Aun scan of [l-Leu11-OMe]-trichogin GA IV, a membrane active synthetic precursor of the natural lipopeptaibol

J Pept Res. 2001 Oct;58(4):317-24. doi: 10.1034/j.1399-3011.2001.00919.x.

Abstract

We synthesized using solution-phase methods three analogs of [l-Leu11-OMe] trichogin GA IV, a membrane active synthetic precursor of the lipopeptaibol antibiotic in which the N-terminal n-octanoyl group and each of the three Aib residues in positions 1, 4 and 8 are replaced by an acetyl group and the lipophilic Calpha,alpha-disubstituted glycine l-(alphaMe)Aun, respectively [partial (alphaMe)Aun scan]. FT-IR absorption and CD analyses unequivocally show that the main three-dimensional structural features of [l-Leu11-OMe] trichogin GA IV are preserved in the analogs. Also, [l-Leu11-OMe] trichogin GA IV and the three Nalpha-acetylated l-(alphaMe)Aun analogs exhibit strictly comparable membrane-modifying properties. Taken together, these results strongly favor the conclusion that a shift of the long hydrocarbon moiety from the Nalpha-blocking group to the side-chain of the 1, 4 or 8 residue does not have any significant effect on the conformational properties or the membrane activity of [l-Leu11-OMe] trichogin GA IV and, by extension, of the natural lipopeptaibol.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-Bacterial Agents / chemical synthesis*
  • Anti-Bacterial Agents / chemistry*
  • Circular Dichroism
  • Glycopeptides
  • Hydrocarbons / chemistry*
  • Lipopeptides
  • Lipoproteins / chemistry*
  • Membranes / chemistry
  • Molecular Conformation
  • Peptides*
  • Solutions / chemistry
  • Spectroscopy, Fourier Transform Infrared
  • Surface-Active Agents / chemical synthesis
  • Water / chemistry

Substances

  • Anti-Bacterial Agents
  • Glycopeptides
  • Hydrocarbons
  • Lipopeptides
  • Lipoproteins
  • Peptides
  • Solutions
  • Surface-Active Agents
  • trichogin GA IV
  • Water