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Molecules 2017, 22(9), 1548; doi:10.3390/molecules22091548

Development of a Non-Hydroxamate Dual Matrix Metalloproteinase (MMP)-7/-13 Inhibitor

Center for Organic and Medicinal Chemistry, Institute of Chemistry and Biotechnology, Zurich University of Applied Sciences ZHAW, Einsiedlerstrasse 31, 8820 Wädenswil, Switzerland
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Received: 26 August 2017 / Revised: 8 September 2017 / Accepted: 8 September 2017 / Published: 14 September 2017
(This article belongs to the Special Issue Metalloenzyme Inhibitors and Activators)
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Abstract

Matrix metalloproteinase 7 (MMP-7) is a member of the MMP superfamily and is able to degrade extracellular matrix proteins such as casein, gelatin, fibronectin and proteoglycan. MMP-7 is a validated target for the development of small molecule drugs against cancer. MMP-13 is within the enzyme class the most efficient contributor to type II collagen degeneration and is a validated target in arthritis and cancer. We have developed the dual MMP-7/-13 inhibitor ZHAWOC6941 with IC50-values of 2.2 μM (MMP-7) and 1.2 μM (MMP-13) that is selective over a broad range of MMP isoforms. It spares MMP-1, -2, -3, -8, -9, -12 and -14, making it a valuable modulator for targeted polypharmacology approaches. View Full-Text
Keywords: matrix metalloproteinase inhibitor; polypharmacology; organic synthesis; drug discovery; structure activity relationship matrix metalloproteinase inhibitor; polypharmacology; organic synthesis; drug discovery; structure activity relationship
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Fischer, T.; Riedl, R. Development of a Non-Hydroxamate Dual Matrix Metalloproteinase (MMP)-7/-13 Inhibitor. Molecules 2017, 22, 1548.

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