Samu Melkko; Yixin Zhang; Christoph E. Dumelin; Jörg Scheuermann; Dario Neri
Angew. Chem. Int. Ed. Engl., 2007, 46(25), 4671-4
https://doi.org/10.1002/anie.200700654

Abstract

Maturing is easy to do: Annealing benzamidine-oligonucleotide conjugates with a library of DNA-encoded compounds allows the affinity capture of pharmacophores that are capable of binding to exosites adjacent to the primary substrate-binding pocket of the serine protease trypsin. Selected conjugates show an improvement in IC50 values of several orders of magnitude compared with the starting benzamidine.