DNA-encoded chemical libraries for the discovery of MMP-3 inhibitors |
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Authors: | Scheuermann Jörg Dumelin Christoph E Melkko Samu Zhang Yixin Mannocci Luca Jaggi Madalina Sobek Jens Neri Dario |
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Affiliation: | Institute of Pharmaceutical Sciences, Department of Chemistry and Applied Biosciences, ETH Zürich, Wolfgang-Pauli-Strasse10, CH-8093 Zurich, Switzerland. |
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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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