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Title: Development of a non-hydroxamate dual matrix metalloproteinase (MMP)-7/-13 inhibitor
Authors : Fischer, Thomas
Riedl, Rainer
Published in : Molecules : a Journal of Synthetic Organic and Natural Product Chemistry
Volume(Issue) : 22
Issue : 9/1548
Publisher / Ed. Institution : MDPI
Issue Date: 2017
Language : Englisch / English
Subjects : Medicinal chemistry; Drug discovery; Inhibitor
Subject (DDC) : 615: Pharmakologie und Therapeutik
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 M (MMP-7) and 1.2 M (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.
Departement: Life Sciences und Facility Management
Publication type: Beitrag in wissenschaftlicher Zeitschrift / Article in scientific Journal
Type of review: Peer review (Publikation)
DOI : 10.3390/molecules22091548
ISSN: 1420-3049
License (according to publishing contract) : CC BY 4.0: Namensnennung 4.0 International
Appears in Collections:Publikationen Life Sciences und Facility Management

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