Biosynthesis of triacsin featuring an N-hydroxytriazene pharmacophore

Nat Chem Biol. 2021 Dec;17(12):1305-1313. doi: 10.1038/s41589-021-00895-3. Epub 2021 Nov 1.

Abstract

Triacsins are an intriguing class of specialized metabolites possessing a conserved N-hydroxytriazene moiety not found in any other known natural products. Triacsins are notable as potent acyl-CoA synthetase inhibitors in lipid metabolism, yet their biosynthesis has remained elusive. Through extensive mutagenesis and biochemical studies, we here report all enzymes required to construct and install the N-hydroxytriazene pharmacophore of triacsins. Two distinct ATP-dependent enzymes were revealed to catalyze the two consecutive N-N bond formation reactions, including a glycine-utilizing, hydrazine-forming enzyme (Tri28) and a nitrite-utilizing, N-nitrosating enzyme (Tri17). This study paves the way for future mechanistic interrogation and biocatalytic application of enzymes for N-N bond formation.

Publication types

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

MeSH terms

  • Biocatalysis
  • Coenzyme A Ligases / metabolism*
  • Escherichia coli / genetics
  • Glycine / chemistry
  • Hydrazines / chemistry
  • Lipid Metabolism
  • Lipids / chemistry
  • Nitrites / chemistry
  • Streptomyces aureofaciens / enzymology*
  • Streptomyces aureofaciens / genetics*
  • Triazenes / chemistry
  • Triazenes / metabolism*

Substances

  • Hydrazines
  • Lipids
  • Nitrites
  • Triazenes
  • hydrazine
  • Coenzyme A Ligases
  • long-chain-fatty-acid-CoA ligase
  • Glycine