Target-guided synthesis (TGS) of enzyme inhibitors via a two-component cyclocondensation using urokinase plasminogen activator (uPA) as a model target. University of Antwerp
Common to all contemporary drug discovery strategies is that they revolve around iterative cycles of design, synthesis and potency evaluation, each time producing further optimized compounds. This is generally a very time- and cost-consuming process that could be significantly shortened by implementing so-called target-guided synthesis (TGS). The latter relies on direct assistance of the drug target, which serves as a physical template that ...