Molecular evolution of a steroid hydroxylating cytochrome P450 using a versatile steroid detection system for screening

Lipids. 2008 Dec;43(12):1133-41. doi: 10.1007/s11745-008-3236-8. Epub 2008 Oct 1.

Abstract

Molecular evolution is a powerful tool for improving or changing activities of enzymes for their use in biotechnological processes. Cytochromes P450 are highly interesting enzymes for biotechnological purposes because they are able to hydroxylate a broad variety of substrates with high regio- and stereoselectivity. One promising steroid hydroxylating cytochrome P450 for biotechnological applications is CYP106A2 from Bacillus megaterium ATCC 13368. It is one of a few known bacterial cytochromes P450 able to transform steroids such as progesterone and 11-deoxycortisol. CYP106A2 can be easily expressed in Escherichia coli with a high yield and can be reconstituted using the adrenal redox proteins, adrenodoxin and adrenodoxin reductase. We developed a simple screening assay for this system and performed random mutagenesis of CYP106A2, yielding variants with improved 11-deoxycortisol and progesterone hydroxylation activity. After two generations of directed evolution, we were able to improve the k (cat)/K (m) of the 11-deoxycortisol hydroxylation by a factor of more than four. At the same time progesterone conversion was improved about 1.4-fold. Mapping the mutations identified in catalytically improved CYP106A2 variants into the structure of a CYP106A2 model suggests that these mutations influence the mobility of the F/G loop, and the interaction with the redox partner adrenodoxin. The results show the evolution of a soluble steroid hydroxylase as a potential new catalyst for the production of steroidogenic compounds.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adrenodoxin / genetics
  • Adrenodoxin / metabolism
  • Bacillus megaterium / enzymology
  • Bacterial Proteins / chemistry
  • Bacterial Proteins / genetics*
  • Bacterial Proteins / metabolism*
  • Biological Assay / methods*
  • Cortodoxone / chemistry
  • Cortodoxone / metabolism
  • Cytochrome P-450 Enzyme System / chemistry
  • Cytochrome P-450 Enzyme System / genetics*
  • Cytochrome P-450 Enzyme System / metabolism*
  • Directed Molecular Evolution*
  • Ferredoxin-NADP Reductase / genetics
  • Ferredoxin-NADP Reductase / metabolism
  • Models, Molecular
  • Mutagenesis
  • Protein Structure, Tertiary
  • Steroids* / chemistry
  • Steroids* / metabolism

Substances

  • Bacterial Proteins
  • Steroids
  • Adrenodoxin
  • Cytochrome P-450 Enzyme System
  • 15beta-hydroxylase CYP106A2, Bacillus megaterium
  • Ferredoxin-NADP Reductase
  • Cortodoxone