Status of protein engineering for biocatalysts: how to design an industrially useful biocatalyst

Curr Opin Chem Biol. 2011 Apr;15(2):194-200. doi: 10.1016/j.cbpa.2010.11.011. Epub 2010 Nov 27.


Recent advances in the development of both experimental and computational protein engineering tools have enabled a number of further successes in the development of biocatalysts ready for large-scale applications. Key tools are first, the targeting of libraries, leading to far smaller but more useful libraries than in the past, second, the combination of structural, mechanistic, and sequence-based knowledge often based on prior successful cases, and third, the advent of structurally based algorithms allowing the design of novel functions. Based on these tools, a number of improved biocatalysts for pharmaceutical applications have been presented, such as an (R)-transaminase for the synthesis of active pharmaceutical ingredients (APIs) of sitagliptin (Januvia®) and ketoreductases, glucose dehydrogenases, and haloalkane dehalogenases for the API synthesis toward atorvastatin (Lipitor®) and montelukast (Singulair®).

Publication types

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

MeSH terms

  • Animals
  • Biocatalysis*
  • Computational Biology / methods
  • Computational Biology / trends*
  • Humans
  • Models, Molecular
  • Protein Engineering / methods
  • Protein Engineering / trends*
  • Proteins / chemistry
  • Proteins / genetics
  • Proteins / metabolism


  • Proteins