BUSINESS WIRE; Monday, June 29, 1998
The results were presented in Geneva at the International AIDS Conference by Gryphon's collaborator, Dr. Donald Mosier of The Scripps Research Institute. The chemical protein analogue Nonanoyl-RANTES was developed using Gryphon's chemical protein synthesis technology, applying the principles of medicinal chemistry to AOP-RANTES as a "lead protein."
AOP-RANTES was first reported as an HIV inhibitor in the April 11, 1997, issue of Science. Dr. Mosier tested both AOP-RANTES and Nonanoyl-RANTES in the hu-PBL-SCID model. At very low (100 femtomolar) concentrations nonanoyl RANTES was strongly protective. By contrast, the AOP-RANTES was minimally protective at 500 femtomolar concentrations in the same model.
"These are exciting results," said Dr. Mosier, "because it is the first demonstration of a CCR5 antagonist working in an accepted in vivo model of AIDS. Approximately 60 percent of the animals were protected, and we have not seen 'escape mutants' in the few animals that became infected. That's a big step in the right direction toward a new AIDS therapeutic."
These results showcase the power of Gryphon's Chemical Protein Synthesis technology for rapidly accelerating drug discovery. Dr. Stephen Kent, president and chief scientist at Gryphon, states: "These results demonstrate that chemical protein synthesis can be used effectively to apply the principles of medicinal chemistry to a protein lead molecule. It's simply not practical and in many cases not possible to make such molecules by other technologies.
"The insight gained in studying the mechanism of action of this molecule should lead to a better understanding of the structure-function activities of these important molecular players in a major disease. That will lead to better drugs. Furthermore, by using Gryphon's chemical protein synthesis technology to design and produce unique protein molecules with improved properties, it will be possible to find proprietary new protein therapeutics. In a pharmaceutical industry looking for important drugs, chemical protein synthesis can provide a major competitive advantage."
Gryphon Sciences' powerful Chemical Protein Synthesis technology can be used to produce proteins directly from genome data for use in drug discovery. The technology provides direct access to function from the gene sequence, thereby greatly accelerating the drug discovery process. Gryphon uses proprietary chemical technologies to stitch together peptide segments covering the entire sequence encoded by the gene, thus making the target protein's polypeptide chain.
The resulting protein displays the full range of biological activities encoded in the gene. Gryphon's proprietary chemistries also enable the rapid preparation of pure proteins in precisely labeled forms for use in drug screening. Gryphon is commercializing its proprietary technology through discovery and development collaborations with large pharmaceutical and biotechnology companies, and with genomics tool companies.
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CONTACT: Gryphon Sciences Janice M. LeCocq, 650/952-7714 www.gryphonsci.com
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