LA JOLLA, Calif., March 17 /PRNewswire/ -- 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.
Insights gained from the three-dimensional structure will be 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, 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.
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CONTACT:
Joy Schmitt, Director, Product Public
Relations, Agouron Pharmaceuticals, Inc., 858-622-3220
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