DNA-Encoded Chemical Libraries for the Discovery of MMP-3 Inhibitors
Bioconjugate Chemistry2008Vol. 19(3), pp. 778–785
Citations Over TimeTop 10% of 2008 papers
Jörg Scheuermann, Christoph E. Dumelin, Samu Melkko, Yixin Zhang, Luca Mannocci, Madalina Jaggi, Jens Sobek, Dario Neri
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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