Agouron Solves Structure of Key Target for Oncology: Checkpoint Kinase I
LA JOLLA, Calif., March 17, 2000 -- Agouron Pharmaceuticals, Inc. today announced that its scientists have solved the atomic structure of a protein which plays a critical role in cell cycle regulation. This protein, checkpoint kinase I (Chk1), is pivotal in a step of cellular regulation that protects cancer cells from damage caused by chemotherapy and radiation, common anticancer treatments. The structure of Chk1, determined by x-ray crystallography to a resolution of 1.7 Angstroms, is being reported in today's edition of the scientific journal Cell. The discovery is expected to contribute importantly to the development of new drugs for treatment of cancer.
A used to guide discovery of drugs that inhibit Chk1. Agouron scientists are presently engaged in the design, synthesis, and evaluation of inhibitors based upon this structure.
"The crystal structure of Chk1 provides a significant advantage in designing highly selective inhibitors of this important cancer target. Chk1 inhibition affords the potential for broad application in a large number of different human tumor treatment settings. The solution of this structure by Agouron scientists is an important and timely example of the progress resulting from our commitment to novel anti-tumor strategies," said Patrick O'Connor, Ph.D., vice-president, head of oncology research.
Compounds emerging from the Chk1 program will join a strong portfolio of agents directed at a range of targets identified within Agouron's oncology programs. The cancer research and development program is focused on novel therapeutics that inhibit the mechanisms of angiogenesis, signal transduction, and cell cycle control. Prinomastat, a matrix metalloprotease (MMP) inhibitor, is in Phase III clinical trials in combination therapy for hormone-refractory prostate cancer and non-small cell lung cancer (see, update Phase III Clinical Trial of Prinomastat Halted, Aug 2000) and a Phase II trial for glioblastoma multiforme (a specific type of brain tumor).
Agouron Pharmaceuticals, Inc., a wholly owned subsidiary of the Warner-Lambert Company (NYSE: WLA), is an integrated pharmaceutical company committed to the discovery, development, manufacturing, and marketing of innovative therapeutic products engineered to inactivate proteins that play key roles in cancer, AIDS, and other serious diseases. Agouron employs more than 1200 people of whom approximately 800 are engaged in research and development.
SOURCE Agouron Pharmaceuticals, Inc.
Web Site: http://www.agouron.com
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