Cengent Therapeutics, a structure-guided drug discovery company, announced the signing of a Genes-to-Leads drug discovery contract with the Novartis Institutes for BioMedical Research site in Basel, Switzerland (Novartis Pharma AG). Under the agreement, Cengent will apply its proprietary structure-based lead identification technology to screen for drug candidates against multiple targets identified by the Novartis Institutes.

Financial terms were not disclosed, but include up-front and milestone payments.

Genes To Leads is a compound lead generation service that greatly accelerates and optimizes drug discovery. Using an identified drug target, Genes To Leads selects closely related structural proteins (anti-targets) for analysis using complementary structure-based and sequence-based methods.

This analysis of targets and anti-targets incorporates selectivity into identified leads, improving odds of a successful lead optimization candidate. Differential dynamic pharmacophores are defined for the protein target and anti-targets by analyzing the flexibility of putative binding sites. The functional relationships required for a ligand to bind are better defined from this dynamic pharmacophoric analysis of both targets and anti-targets. Finally, a query that can be used to search commercial compound databases, proprietary databases, or virtual databases is generated with results filtered to match customer requirements. This process provides maximum flexibility to the customer in terms of scope of compound search as well as "hit" requirements.

Genes To Leads technology has been successfully applied to 15 targets on a contract basis for a growing number of pharmaceutical and biotech companies, and as the basis for Cengent's own highly successful in house programs for orally active PTP-1B inhibitors (for treatment of type II diabetes and obesity) and anthrax lethal factor inhibitors.