Molecules (Basel, Switzerland), 2017-09, Vol.22 (9), p.1548
2017
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Details
- Autor(en) / Beteiligte
- Titel
- Development of a Non-Hydroxamate Dual Matrix Metalloproteinase (MMP)-7/-13 Inhibitor
- Ist Teil von
- Molecules (Basel, Switzerland), 2017-09, Vol.22 (9), p.1548
- Ort / Verlag
- Basel: MDPI AG
- Erscheinungsjahr
- 2017
- Quelle
- EZB Electronic Journals Library
- Beschreibungen/Notizen
- 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.
- Sprache
- Englisch
- Identifikatoren
- ISSN: 1420-3049eISSN: 1420-3049DOI: 10.3390/molecules22091548Titel-ID: cdi_doaj_primary_oai_doaj_org_article_0dadc9cb975e4eebb7ca976bcae6dbe0
- Format
- –
- Schlagworte
- Arthritis, Cancer, Cancer therapies, Casein, Codes, Collagen (type II), Collagenase 3, Degeneration, Drug development, drug discovery, Drugs, Enzymes, Extracellular matrix, Fibronectin, Gelatin, Inhibitors, Interstitial collagenase, Isoforms, Ligands, Matrilysin, Matrix metalloproteinase, matrix metalloproteinase inhibitor, Metalloproteinase, organic synthesis, polypharmacology, Proteins, structure activity relationship