SAN DIEGO -- Agouron Pharmaceuticals Inc. reported todaythat its scientists have discovered the three-dimensionalatomic structure of an enzyme involved in the rapidproliferation of cancer cells. The discovery is expected to helpin the design of novel drugs to treat malignant tumors, thecompany said.

In today's edition of the Proceedings of the National Academyof Sciences, Agouron researchers report on an enzyme calledglycinamide ribonucleotide transformylase (GART). It isrequired for the biosynthesis of purine nucleotides that areessential building blocks of DNA.

Inhibiting the enzyme has been shown to deprive rapidlyproliferating cancer cells of their ability to synthesize new DNA,which is required to sustain their explosive growth rate.

"It opens the door to rational design of anti-cancer drugs," saidDonna Nichols, Agouron's manager of corporatecommunications. She said it will be easier to create novel anti-cancer drugs because "we know exactly what the atoms are andexactly what the three-dimensional structure (of GART) is."

As part of a four-year agreement, Agouron and Eli Lilly and Co.of Indianapolis are using the discovery to co-develop novelinhibitors of GART. Nichols said Agouron intends to file initialpatent applications on compounds that use the GART structureto halt the growth of cultured tumor cells in vitro.

-- Steve Payne BioWorld Staff

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