Cell-free synthesis of polyketides by recombinant erythromycin polyketide synthases

Nature. 1995 Nov 16;378(6554):263-6. doi: 10.1038/378263a0.

Abstract

Modular polyketide synthases (PKSs) are complex multi-enzyme proteins that catalyse the bacterial biosynthesis of many pharmaceutically useful polyketides. The PKSs are organized into a series of modules, each containing the active catalytic sites required for one step in the synthesis process. Here we report a method for cell-free enzymatic synthesis of 6-deoxyerythronolide B (6-dEB), the parent molecule of the antibiotic erythromycin A, using recombinant 6-deoxyerythronolide B synthase (DEBS), a modular PKS with at least 28 distinct active sites. We have also synthesized in vitro a triketide lactone by using a truncated mutant of DEBS. The availability of such cell-free synthetic routes will allow direct investigation of the structural and mechanistic basis for the unusual combination of high substrate specificity and tolerance to genetic reprogramming found in this enzyme family.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, Non-P.H.S.
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Amino Acid Sequence
  • Cell-Free System
  • Erythromycin / analogs & derivatives*
  • Erythromycin / biosynthesis
  • Molecular Sequence Data
  • Multienzyme Complexes / genetics
  • Multienzyme Complexes / metabolism*
  • Pyrones / metabolism
  • Recombinant Proteins / genetics
  • Recombinant Proteins / metabolism
  • Sequence Deletion
  • Streptomyces

Substances

  • 2,4-dimethyl-3,5-dihydroxy-n-heptanoic acid delta lactone
  • Multienzyme Complexes
  • Pyrones
  • Recombinant Proteins
  • 6-deoxyerythronolide B
  • Erythromycin