Antimicrobials Inspired by Nonribosomal Peptide Synthetase Gene Clusters

J Am Chem Soc. 2017 Feb 1;139(4):1404-1407. doi: 10.1021/jacs.6b11861. Epub 2017 Jan 23.

Abstract

Bacterial culture broth extracts have been the starting point for the development of numerous therapeutics. However, only a small fraction of bacterial biosynthetic diversity is accessible using this strategy. Here, we apply a discovery approach that bypasses the culturing step entirely by bioinformatically predicting small molecule structures from the primary sequences of the biosynthetic gene clusters. These structures are then chemically synthesized to give synthetic-bioinformatic natural products (syn-BNPs). Using this approach, we screened syn-BNPs inspired by nonribosomal peptide synthetases against microbial pathogens, and discovered an antibiotic for which no resistance could be identified and an antifungal agent with activity against diverse fungal pathogens.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Anti-Bacterial Agents / chemistry
  • Anti-Bacterial Agents / metabolism
  • Anti-Bacterial Agents / pharmacology*
  • Antifungal Agents / chemistry
  • Antifungal Agents / metabolism
  • Antifungal Agents / pharmacology*
  • Bacteria / drug effects*
  • Biological Products / chemistry
  • Biological Products / metabolism
  • Biological Products / pharmacology*
  • Computational Biology
  • Fungi / drug effects*
  • Microbial Sensitivity Tests
  • Multigene Family
  • Peptide Synthases / genetics*
  • Peptide Synthases / metabolism

Substances

  • Anti-Bacterial Agents
  • Antifungal Agents
  • Biological Products
  • Peptide Synthases
  • non-ribosomal peptide synthase