AGOURON SOLVES STRUCTURE OF CANCER-RELATED ENZYME
AGOURON SOLVES STRUCTURE OF CANCER-RELATED ENZYME SAN DIEGO, July 1 /PRNewswire/ -- Agouron Pharmaceuticals Inc.
(NASDAQ-NMS: AGPH) today announced that its scientists have solved the three-dimensional atomic structure of an enzyme involved in the rapid proliferation of cancer cells. The discovery is expected to facilitate the design of novel drugs for treatment of malignant tumors.
In the July 1, 1992 issue of the "Proceedings of the National Academy of Sciences," Vol. 89, No. 13, Agouron scientists report they have employed the techniques of X-ray crystallography to solve the three-dimensional atomic structure of a protein known as glycinamide ribonucleotide transformylase (GART). GART is an enzyme required for the biosynthesis of purine nucleotides -- essential building blocks of DNA. Inhibition of GART by such drugs as the investigational anti-tumor agent lometrexol, currently being developed by Eli Lilly and Co., is known to deprive rapidly proliferating cancer cells of their ability to synthesize the new DNA required to sustain their explosive rate of growth. In addition to the solution of the GART structure, the Agouron scientists also report in today's P.N.A.S. article that they have used X-ray crystallography to determine at the atomic level how such drugs as lometrexol interact with GART to shut off its normal activity. Scientists from Agouron and Lilly are now engaged in a Lilly-sponsored joint effort to exploit these discoveries in the design of novel inhibitors of GART with pharmacological properties different from those of lometrexol or other existing drugs. Agouron's investigation of the GART structure was undertaken as part of the Agouron-Lilly collaborative research and development program. Agouron research reported today was conducted using GART enzyme from bacteria. Agouron confirmed that in research yet to be published, its scientists have also solved the structure of GART in the form in which it occurs in humans. Agouron Pharmaceuticals Inc. is a pioneer and leader of a new technology for the rational design of novel synthetic drugs based upon the molecular structures of proteins which play key roles in human disease. Agouron is currently applying this technology to the design and development of drugs for treatment of cancer, AIDS and other serious diseases. -0- 7/1/92 /CONTACT: Peter Johnson, president and CEO, or Donna Nichols of Agouron Pharmaceuticals, 619-622-3000/ (AGPH) CO: Agouron Pharmaceuticals Inc. ST: California IN: MTC SU:
KJ-EH -- SD003 -- 5516 07/01/92 09:03 EDT
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|Date:||Jul 1, 1992|
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