DGI of course claimed success, but not using molecule-guided binding of the "epitopes" to a template, long ago. We've discussed Sunesis here before. If they can do this -- map multiple pharmacophore binding sites and then use the macromolecule as a template -- it's a big-time advance in the future of medicine.......
Sunesis Announces Breakthrough In Lead Discovery Technology Using Extended Tethering
Wednesday February 5, 8:32 am ET
Findings Highlighted in Advance Online Publication of Nature Biotechnology
SOUTH SAN FRANCISCO, Calif., Feb. 5 /PRNewswire/ -- Sunesis Pharmaceuticals, Inc. announced today a novel drug discovery technology for the rapid, efficient identification of enzyme inhibitor molecules. The research program is directed at Caspases, an important group of proteases involved in the modulation of major apoptotic and inflammatory diseases. The results of this research are available in an advance online publication ("In situ assembly of enzyme inhibitors using extended tethering") of Nature Biotechnology, an abstract of which can be found at dx.doi.org.
James Wells, Ph.D., President and Chief Scientific Officer of Sunesis, commented, "This program has provided an excellent demonstration of Extended Tethering, a powerful approach to finding novel companion ligands that are tethered directly to a core binding pharmacophore. The resulting linked compounds provide the basis for moving rapidly into lead optimization. The key to this breakthrough is that we use the biological target molecule as the template for the in-situ construction of its own inhibitor within the target's active site."
Dr. Wells continued, "In the work described in this publication, we identified tight-binding, small molecules that inhibit Caspase-3 and modulate apoptosis in cells. We have recently expanded our research efforts towards Caspase-1, an intracellular enzyme associated with inflammatory diseases including asthma and rheumatoid arthritis. In addition to proteases, we believe Extended Tethering can be applied to many other important target families, such as kinases and phosphatases."
Sunesis Technology Overview
Sunesis' fragment-based discovery platform reliably generates novel hits against challenging targets by identifying binding ligands that other techniques such as high-throughput screening are too insensitive to find. Sunesis scientists screen libraries of fragments, fundamental building blocks of oral therapeutics, against validated targets that have been resistant to small molecule discovery. The basis for this approach is Tethering, a process in which the protein target selects fragments with binding affinity for a specific region on its surface. By discovering drugs in pieces, Sunesis can efficiently search a chemical diversity space equivalent to hundreds of millions of compounds.
About Sunesis
Sunesis is a leading discovery-based pharmaceutical company that applies its breakthrough fragment-based technologies to create superior oral therapeutics for the most challenging and important disease targets. Sunesis is building a pipeline of innovative therapeutics addressing major diseases through internal development and selective partnering.
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Source: Sunesis Pharmaceuticals, Inc. |
