Molecules2017,Vol.22Issue(9) :27.DOI:10.3390/molecules22091548

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

Fischer, Thomas Riedl, Rainer
Molecules2017,Vol.22Issue(9) :27.DOI:10.3390/molecules22091548

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

Fischer, Thomas 1Riedl, Rainer1
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作者信息

  • 1. Zurich Univ Appl Sci ZHAW, Inst Chem & Biotechnol, Ctr Organ & Med Chem, Einsiedlerstr 31, CH-8820 Wadenswil, Switzerland
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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 mu M (MMP-7) and 1.2 mu 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.

Key words

matrix metalloproteinase inhibitor/polypharmacology/organic synthesis/drug discovery/structure activity relationship

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出版年

2017
Molecules

Molecules

SCI
ISSN:1420-3049
被引量6
参考文献量49
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