World first discovery of novel enzyme

Thursday 21 March 2002

Scientists in Scotland have discovered the World’s first fluorinase enzyme, a biological catalyst which bonds carbon to fluorine, which will be useful for creating compounds as diverse as Teflon and Prozac.

The discovery, patent-pending, is published in the latest issue of the international journal Nature and has been made by Professor David O’Hagan and his research colleagues at the University of St Andrews.

Fluorine-containing molecules are extremely important commercial entities and their significance continues to grow. Well known compounds in this category include the non-stick polymer Teflon, the antidepressant Prozac and the cancer chemotherapy agent 5- fluorouracil.

“Clearly the discovery of a biochemical ‘first’ is exciting but the identification of the fluorinase opens up possibilities of preparing biologically significant fluorinated compounds using a biocatalyst in place of chemical methods,” said Professor O’Hagan.

“The challenge now is to overexpress the protein and make the catalyst available to researchers worldwide,” he continued.

Professor O’Hagan, a Professor of Organic Chemistry, made the finding with his colleagues, Christoph Schaffrath and Dr Cormac Murphy at the University’s Centre for Biomolecular Sciences.

There is an increasing requirement for novel methods to make complex fluorinated compounds particularly for pharmaceutical development. In the area of pharmaceutical discovery alone, the years between 1980 to 2000 have seen the number of fluorine containing compounds entering clinical trials rise from 8% to the current figure of 16%.

As the 13th most abundant element, fluorine is very plentiful on the earths crust. However, it is tied up as insoluble fluoride minerals and the available fluoride in sea and surface water is very low (about 10 thousand times less than chloride). As a consequence nature has hardly developed a biochemistry of fluorine and there are very few naturally occurring fluorinated compounds.

“The discovery of the fluorinase is a very rare and happy find as it offers fluorine chemists a novel and environmentally neutral (biotechnological) method for the synthesis of organo-fluorine compounds,” said Professor O’Hagan.



Dr Cormac Murphy is a BBSRC (Biotechnology and Biological Sciences Research Council) funded Research Assistant, and Christoph Schaffrath is a PhD student at the University of St Andrews.


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