Elucidation of the Cryptic Methyl Group Epimerase Activity of Dehydratase Domains from Modular Polyketide Synthases Using a Tandem Modules Epimerase Assay

J Am Chem Soc. 2017 Jul 19;139(28):9507-9510. doi: 10.1021/jacs.7b05502. Epub 2017 Jul 7.

Abstract

Dehydratase (DH) domains of cryptic function are often found in polyketide synthase (PKS) modules that produce epimerized (2S)-2-methyl-3-ketoacyl-ACP (acyl carrier protein) intermediates. A combination of tandem equilibrium isotope exchange (EIX) and a newly developed Tandem Modules Epimerase assay revealed the intrinsic epimerase activity of NanDH1 and NanDH5, from modules 1 and 5, respectively, of the nanchangmycin (1) PKS as well of NigDH1, from module 1 of the nigericin (3) PKS. Unexpectedly, all three epimerase-active DH domains were also found to possess intrinsic dehydratase activity, whereas the conventional DH domains, EryDH4, from module 4 of the erythromycin synthase, and NanDH2 from module 2 of the nanchangmycin synthase, were shown to have cryptic epimerase activity.

Publication types

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

MeSH terms

  • Enzyme Assays*
  • Hydro-Lyases / chemistry
  • Hydro-Lyases / metabolism*
  • Molecular Structure
  • Polyketide Synthases / chemistry
  • Polyketide Synthases / metabolism*
  • Protein Domains
  • Racemases and Epimerases / chemistry
  • Racemases and Epimerases / metabolism*

Substances

  • Polyketide Synthases
  • Hydro-Lyases
  • Racemases and Epimerases