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Biotech / Medical : Trickle Portfolio -- Ignore unavailable to you. Want to Upgrade?

To: tuck who wrote (869)	10/29/2001 9:43:06 AM
From: tuck	Respond to of 1784

>>CHICAGO, Oct. 29 /PRNewswire/ -- MediChem Life Sciences (Nasdaq: MCLS - news), a Chicago-based drug discovery technology and services company, announced today that Emerald BioStructures, its structural proteomics division, was awarded a phase II Small Business Innovation Research (SBIR) grant from the National Cancer Institute (NCI) to conduct structure-based drug design of anti-cancer compounds targeting human DNA topoisomerase I. ``Using Phase I grant funding, we solved the X-ray crystal structures of a variety of known anti-cancer compounds bound to human topoisomerase I in complex with DNA. With Phase II funding, we are using this unique structural information to design, synthesize and test a series of completely novel anti-cancer drugs,'' said Lance Stewart, Ph.D. principal investigator and president of Emerald BioStructures. The $750,000 SBIR award from the NCI supports the first year of a two-year program. Additional funding is expected for the second year. An interdisciplinary team of MediChem researchers, who have expertise in biochemistry, crystallography, computational chemistry and medicinal chemistry, will perform the anti-cancer drug design. ``This project leverages our unique capabilities in protein crystallography with our expertise in the design and synthesis of novel drug molecules,'' said Michael T. Flavin, Ph.D., MediChem's president and CEO. ``The funding represents a peer reviewed validation of our structural proteomics platform for drug discovery and will allow us to execute a full cycle structure-based anti-cancer drug development program.'' Topoisomerase I is an essential nuclear enzyme that relaxes tension in DNA by transiently breaking one strand of the double helix. Anti-cancer drugs such as Hycamtin (TM) and Camptosar (TM), both of which are FDA-approved analogues of the natural product camptothecin, convert topoisomerase I into a DNA damaging agent by preventing the enzyme from resealing the breaks it generates. Many cancer cells are particularly sensitive to the toxic effects of topoisomerase I inhibitors which trigger the cancer cells to undergo programmed cell death. MediChem Life Sciences has a strong track record in the development of new topoisomerase I inhibitors. The company has received six SBIR grants from the NCI for the design and synthesis of novel camptothecin and indolocarbazole analogues, as well as the X-ray crystal structure determination of such compounds bound to topoisomerase I. The company is uniquely positioned to provide pharmaceutical partners with new anti-cancer compounds that target this enzyme. MediChem's subsidiary, Emerald BioStructures, is a leader in the field of structural proteomics, and has developed a series of robotic high-throughput crystallization (RoboHTC) tools that allow protein-drug co-crystal structures to be solved in an industrialized format. This platform of technologies was used to grow crystals of the ternary topoisomerase I-DNA-drug complexes whose structures revealed precisely how anti-cancer drugs interact with their molecular target.<< snip Cheers, Tuck