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AGOURON REPORTS NOVEL ANTI-HIV COMPOUNDS

 LA JOLLA, Calif., Oct. 20 /PRNewswire/ -- In a presentation at the 33rd Interscience Conference on Antimicrobial Agents and Chemotherapy in New Orleans, Agouron Pharmaceuticals Inc. (NASDAQ-NMS: AGPH) revealed the chemical structure of a novel class of orally bioavailable chemical compounds which potently inhibit a key enzyme required for replication of HIV and which, as a result, halt HIV infection of T lymphocytes in vitro.
 Agouron scientist Krzysztof Appelt, Ph.D., described in atomic detail the de novo design of a previously unknown class of inhibitors of the enzyme HIV protease by a team of Agouron scientists working in cooperation with scientists at Eli Lilly. Guided by x-ray generated snapshots revealing precisely how each new compound in the novel series fits into a critical "active site" cleft on the surface of the enzyme, the Agouron research team incrementally achieved a 60,000-fold enhancement in the potency of the first compound in the series. The result, a compound designated AG1284, inactivated the enzyme with a potency equivalent to that of the most potent inhibitors of HIV protease previously reported. In preclinical in vivo experiments, oral administration of AG1284 resulted in plasma levels of the compound several-fold higher than the minimum concentration required for in vitro anti-HIV activity of the compound.
 Dr. Appelt characterized the results of the research program as a strong testimony to the power of protein structure-based drug design. "We have today presented details of the step-by-step design and optimization of one series of very novel HIV protease inhibitors which we regard as having significant clinical potential," said Dr. Appelt. "But we have used this same protein structure-based design methodology to generate other novel HIV protease inhibitors with completely different chemical structures whose preclinical performance appears to equal or to exceed that of this first series of Agouron compounds or, for that matter, the preclinical performance of any HIV protease inhibitor yet reported by others working in this field. We believe it is in this ability to generate multiple development candidates, each of a completely different chemical character, that the special strength of protein structure-based drug design lies."
 "We are encouraged and excited by the preclinical research results reported today in New Orleans, but we wish to sound a general caution against premature expectations for anti-HIV agents based solely upon preclinical data," said Peter Johnson, the company's president and chief executive officer.
 Agouron Pharmaceuticals Inc. is a pioneer and leader in a 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- 10/20/93
 /CONTACT: Peter Johnson, president and CEO, or Donna Nichols, director, corporate communications, of Agouron Pharmaceuticals, 619-622-3009/
 (AGPH)


CO: Agouron Pharmaceuticals Inc. ST: California IN: MTC SU:

JB-LS -- SD001 -- 4362 10/20/93 08:11 EDT
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Publication:PR Newswire
Date:Oct 20, 1993
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