The goal of this program is to develop a new technology for generating biologically active libraries of compounds for high-throughput screening in drug discovery. This new synthesis method will make it possible to create large numbers of drug-candidate compounds with diverse structures -- many of which are difficult or impossible to produce using other library-synthesis methods. In Phase I, (they) plan to produce eight libraries of compounds. Each library will be created from reactants with structural similarities to ligands for two target receptors -- cannabinoid and K-opioid receptors --and the resulting compounds will be screened for binding to these receptors. Feasibility will be demonstrated if binding is demonstrated in at least 1 in 1000 screened compounds. This would represent an order-of-magnitude improvement over the current """"""""hit rates"""""""" achieved using combinatorial-chemistry techniques. Phase II would be aimed at improving hit rates to at least 1 in 100 compounds through structural elucidation and study of receptor binding versus synthetic conditions. The technology would also be extended to other ligand/receptor systems to demonstrate broad applicability. Due to the strong market demand for improved technologies for use with high-throughput screening techniques, we anticipate a straightforward pathway to commercialization.
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