AEGiS-PRn: Agouron Makes Discovery/Helps Anti-viral Research PRNewswireImportant note: Information in this article was accurate in 1996. The state of the art may have changed since the publication date.
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Agouron Makes Discovery/Helps Anti-viral Research

PR Newswire, 810 Seventh Avenue, New York, NY 10019 - Friday, 18 October 1996


LA JOLLA, Calif., Oct. 18 /PRNewswire/ -- Agouron Pharmaceuticals, Inc., today announced that its scientists have solved the three- dimensional atomic structure of the protease enzyme encoded by the human hepatitis C virus (HCV). HCV is a virus that causes illness that ranges from a mild flu-like disease to progressive liver disease, cirrhosis and primary liver cancer. Solution of the HCV protease structure opens the way to the design of a new class of anti-viral drugs that block the HCV protease and disrupt the HCV life cycle.

The solution by Agouron scientists of the NS3 protease structure from HCV at a resolution of 2.4 Angstroms was reported in today's issue of the scientific journal "Cell," Vol. 87, No. 2. The HCV protease is the fourth viral protease structure to be solved over a period of six years by Agouron scientific teams consisting of molecular biologists, protein biochemists and protein crystallographers.

An Agouron research team solved the structure of the HIV protease in 1990. VIRACEPT (nelfinavir mesylate), an Agouron anti-HIV drug now in pivotal clinical trials was designed on the basis of the HIV protease structure. In 1994, an Agouron scientific team solved the structure of the 3C protease enzyme from rhinovirus -- the most frequent cause of the common cold. Agouron is now carrying out preclinical evaluation and optimization of several potent rhinovirus protease inhibitors and intends to commence development of one such compound in 1997. Six weeks ago, Agouron scientists reported their solution of the structure of the protease encoded by cytomegalovirus (CMV) -- a virus that causes degeneration of vision in immunocompromised patients. A major program to design specific inhibitors of the CMV protease is now in progress at Agouron. Agouron is conducting development of VIRACEPT, as well as design of inhibitors of proteases from CMV and HCV in collaboration with the pharmaceutical division of Japan Tobacco Inc. (JT).

"With the structure of the HCV protease in hand, we know of no other company in the pharmaceutical industry in possession of so deep and diversified a structural data base covering proteases as anti-viral drug targets," said Peter Johnson, Agouron's president and chief executive officer. "As a result we expect that VIRACEPT will ultimately prove to be only the first of a series of viral protease inhibitors from Agouron that make important contributions to anti-viral therapy."

Japan Tobacco, a diversified company with annual revenues in excess of $30 billion and assets exceeding $18 billion, entered the pharmaceutical business in 1987. In the field of ethical pharmaceuticals, JT is currently engaged in clinical development of various drugs, including those for the treatment of dimentia, asthma, and angina pectoris, and has launched a 5HT3 antagonist as an anti- emetic in Japan in 1994. JT presently conducts drug discovery research at its new Central Pharmaceutical Research Institute in Osaka, Japan.

Agouron Pharmaceuticals, Inc. is a pioneer and leader in the development and application of technologies that enable the atom by atom design of novel synthetic drugs based upon the molecular structures of target proteins which play key roles in human disease. Agouron is currently applying these technologies to the design and development of novel drugs for treatment of cancer, AIDS and other serious diseases.

SOURCE Agouron Pharmaceuticals

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Keywords: PROTEASE; HEPATITIS; HIV; CLINICAL TRIAL; CYTOMEGALOVIRUS; CMV; IMMUNOCOMPROMISED

Copyright (c) 1996/PR NewsWire. Reproduced with permission. Reproduction of this article (other than one copy for personal reference) must be cleared through the Permissions Desk, PR Newswire, 810 Seventh Avenue, New York, NY 10019.KWDprotease;hepatitis;hiv;clinicaltrial;cytomegalovirus;cmv;immunocompromised
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