Agouron overcomes hurdle to develop cancer drugs
March 4, 1999 07:38 PM
LA JOLLA, Calif., March 4 (Reuters) - Biotech company Agouron Pharmaceuticals Inc. AGPH said its researchers have cracked the design of an enzyme that facilitates a process by which cancerous tumors are able to grow and spread.
By cracking the three-dimensional atomic crystal structure of the VEGFR2 kinase, scientists can develop drugs that block angiogenesis, the process by which new blood vessels are formed and can contribute to the spread of cancer.
"By blocking the process of angiogenesis, we aim to starve a tumor of its essential blood supply," Dr. Patrick O'Connor, chief of oncology research.
The VEGFR2 kinase is the central enzyme in the VEGF signaling pathway, a receptor on the surface of a cell that requlates angiogenesis. In the case of cancer, angiogenesis allows a tumor to grow in size and tumor cells to escape through new blood vessels and spread to distant parts of the body.
Warner Lambert WLA on Jan. 26 said it had agreed to buy Agouron in a stock deal valued at the time at $2.1 billion.
Agouron is known for its best-selling anti-AIDS protease inhibitor Viracept.
The company said the structure of the human VEGFR2 kinase was being reported in the scientific journal, Structure.
Not only does angiogenesis contribute to the spread of cancer, but it also facilitates diabetic retinopathy, blindness brought on by diabetes, and macular degeneration.
Agouron researchers are currently designing inhibitors that would interfere with the process by which the enzyme facilitates angiogenesis. "The crystal structure of the VEGFR2 kinase provides a significant advantage in designing highly selective inhibitors of this important cancer target," O'Connor said.
The company also said compounds emerging from this research would contribute to a strong portfolio of agents directed at targets that were similarly identified in Agouron's research in oncology and ophthalmology.
The company said AG3340, a matrix metalloprotease inhibitor which also demonstrates potent anti-angiogenic and anti-metastatic properties, is in Phase III clinical trials. The trials are designed to produce a combination therapy for hormone-refractory prostate cancer and non-small cell lung cancer.
AG3340 is also undergoing phase II clinical trials for the treatment of age-related macular degeneration, the leading cause of blindness in the elderly.
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