Biotransformations

Extending the application fields of biocombinatoric reactions mediated by Laccases

Using biotransformation to improve the characteristics of pharmacological substances

None of the substances on the market can meet all demands concerning efficiency, side effects, bioavailability, and other characteristics relevant for its application. Therefore an ongoing improvement of known bioactive substances is necessary. Part of this project is to test a procedure capable of a gentle and specific modification of the structure of active substances. By use of polyphenoloxidases the characteristics of known substances can be modified in a specific direction by crosslinking with other specifically chosen substances, which are eventually already active themselves.

The advantages of this procedure are:

• Broad substrate spectrum of the enzyme
• Possibility to selectively introduce functional groups
• Possibility to link larger molecular fragments or already known substances
• Modification can be done under gentle conditions (room temperature, in aqueous solution etc.)
• High rate of reaction

Fig. 1 Production of a coloured crosslinked derivative of an anticancer drug by use of laccase

In cooperation with two middle-class companies the practical application of this technology is studied using basic substances with antibiotic activity as well as antitumor activity to produce new highly active derivatives.