Expanding metabolic pathway for de novo biosynthesis of the chiral pharmaceutical intermediate L-pipecolic acid in Escherichia coli

Microb Cell Fact. 2017 Mar 27;16(1):52. doi: 10.1186/s12934-017-0666-0.

Abstract

Background: The six-carbon circular non-proteinogenic compound L-pipecolic acid is an important chiral drug intermediate with many applications in the pharmaceutical industry. In the present study, we developed a metabolically engineered strain of Escherichia coli for the overproduction of L-pipecolic acid from glucose.

Results: The metabolic pathway from L-lysine to L-pipecolic acid was constructed initially by introducing lysine cyclodeaminase (LCD). Next, L-lysine metabolic flux from glucose was amplified by the plasmid-based overexpression of dapA, lysC, and lysA under the control of the strong trc promoter to increase the biosynthetic pool of the precursor L-lysine. Additionally, since the catalytic efficiency of the key enzyme LCD is limited by the cofactor NAD+, the intracellular pyridine nucleotide concentration was rebalanced by expressing the pntAB gene encoding the transhydrogenase, which elevated the proportion of LCD with bound NAD+ and enhanced L-pipecolic acid production significantly. Further, optimization of Fe2+ and surfactant in the fermentation process resulted in 5.33 g/L L-pipecolic acid, with a yield of 0.13 g/g of glucose via fed-batch cultivation.

Conclusions: We expanded the metabolic pathway for the synthesis of the chiral pharmaceutical intermediate L-pipecolic acid in E. coli. Using the engineered E. coli, a fast and efficient fermentative production of L-pipecolic acid was achieved. This strategy could be applied to the biosynthesis of other commercially and industrially important chiral compounds containing piperidine rings.

Keywords: Chiral intermediate biosynthesis; Cofactor engineering; L-Pipecolic acid; Lysine cyclodeaminase; Metabolic engineering.

MeSH terms

  • Ammonia-Lyases / genetics
  • Batch Cell Culture Techniques
  • Escherichia coli / genetics*
  • Escherichia coli / metabolism*
  • Escherichia coli Proteins / genetics
  • Fermentation
  • Gene Expression
  • Glucose / metabolism
  • Metabolic Engineering / methods*
  • Metabolic Networks and Pathways / genetics*
  • NAD / metabolism
  • NADP Transhydrogenases / genetics
  • Pipecolic Acids / chemistry
  • Pipecolic Acids / metabolism*
  • Plasmids
  • Promoter Regions, Genetic

Substances

  • Escherichia coli Proteins
  • Pipecolic Acids
  • NAD
  • NADP Transhydrogenases
  • pntB protein, E coli
  • Ammonia-Lyases
  • lysine cyclodeaminase
  • pipecolic acid
  • Glucose