DNA-encoded chemical libraries for the discovery of MMP-3 inhibitors

Jörg Scheuermann; Christoph E. Dumelin; Samu Melkko; Yixin Zhang; Luca Mannocci; Madalina Jaggi; Jens Sobek; Dario Neri
Bioconjugate Chem., 2008, 19, 3, 778-785
https://doi.org/10.1021/bc7004347

Abstract

Encoded self-assembling chemical (ESAC) libraries are characterized by the covalent display of chemical moieties at the extremity of self-assembling oligonucleotides carrying a unique DNA sequence for the identification of the corresponding chemical moiety. We have used ESAC library technology in a two-step selection procedure for the identification of novel inhibitors of stromelysin-1 (MMP-3), a matrix metalloproteinase involved in both physiological and pathological tissue remodeling processes, yielding novel inhibitors with micromolar potency.

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