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Novel selective MMP-13 inhibitors reduce collagen degradation in bovine articular and human osteoarthritis cartilage explants
Authors:Dorothea Piecha  Jürgen Weik  Heike Kheil  Gabriele Becher  Andreas Timmermann  Andreas Jaworski  Maren Burger  Michael W. Hofmann
Affiliation:(1) Alantos Pharmaceuticals AG, Heidelberg, Germany;(2) Present address: Fresenius Medical Care Deutschland GmbH, Else-Kroener-Strasse 1, 61352 Bad Homburg, Germany;(3) Present address: Affimed Therapeutics AG, Technologiepark, Im Neuenheimer Feld 582, 69120 Heidelberg, Germany;(4) Present address: X2-Pharma GmbH, Im Neuenheimer Feld 584, 69120 Heidelberg, Germany;(5) Present address: Boehringer Ingelheim Pharma GmbH & Co. KG, Binger Str. 173, 55216 Ingelheim am Rhein, Germany;(6) Present address: Bayer Healthcare AG, 42096 Elberfeld, Germany;(7) Present address: Drug Metabolism and Pharmacokinetics, Bioanalytical Section F, Hoffmann-La Roche Ltd, 4070 Basel, Switzerland
Abstract:

Objective  

MMP-13 is highly upregulated in arthritis and therefore strongly implicated in the pathogenesis of osteoarthritis (OA). Selective inhibition of MMP-13 may provide the desired cartilage degradation protection, while overcoming the musculoskeletal toxicity seen with nonselective inhibition of MMPs.
Keywords:
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