Abstract:Fragment-based drug discovery has been established as a powerful method for the assembly of optimized protein ligands. We employed protein-templated ligations, initially for the site-directed detection of low-affinity fragments and subsequently for the identification of potent fragment combinations that are useful as chemical tools [1][2][3][4].Reversible and irreversible reactions have been employed for ligand construction. Here, we will reflect on the reaction scope of protein-catalyzed ligand formation and … Show more
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