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Drug Discovery

Targanta's antibacterial drug discovery platform exploits unique screening technologies to identify chemical inhibitors of essential targets in in vitro enzyme assays as the first step in discovery of broad-spectrum antibacterial drugs. The activities of Targanta's targets fall under the rubric of nucleic acid metabolism.

Targanta has developed a number of in vitro enzyme assays using proprietary technology. Each screen has been optimized to find competitive inhibitors of the target-dependent enzymatic activity.

An additional feature, unique to Targanta, is the availability of antibacterial phage polypeptides that bind to and inactivate their cognate bacterial target. These phage tools support assay development and validate the target-dependent screening assays by virtue of their specificity and tight interactions with their target. Antibacterial phage polypeptides are identified using a proprietary platform which combines large-scale phage genome sequencing, functional genomics, and proteomics approaches to ultimately identify bacterial protein targets that are amenable for small-molecule antibiotic discovery.

Each of Targanta's screening assays represents a rich source of activities and interactions for inhibitor discovery since enzymatic activities, protein-nucleic acid interactions and protein-protein interactions are all present as targets for inhibition. Early-stage molecules from this screening process have been validated by demonstration of antibacterial activity. Targanta characterizes their activity with a range of confirmatory and secondary assays to assess their potential for further development. Targanta increases the potency and spectrum of their antimicrobial activity and minimizes their liabilities through a combination of chemical synthesis of analogs and biological profiling in an iterative manner.