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Serine proteinases in the turnover of the cartilage extracellular matrix in the joint: Implications for therapeutics

Lookup NU author(s): Dr David Wilkinson, Dr Maria Arques Mengual, Emeritus Professor Drew Rowan


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© 2018 The British Pharmacological Society. Cartilage destruction is a key characteristic of arthritic disease, a process now widely established to be mediated by metzincins such as MMPs. Despite showing promise in preclinical trials during the 1990s, MMP inhibitors for the blockade of extracellular matrix turnover in the treatment of cancer and arthritis failed clinically, primarily due to poor selectivity for target MMPs. In recent years, roles for serine proteinases in the proteolytic cascades leading to cartilage destruction have become increasingly apparent, renewing interest in the potential for new therapeutic strategies that utilize pharmacological inhibitors against this class of proteinases. Herein, we describe key serine proteinases with likely importance in arthritic disease and highlight recent advances in this field.

Publication metadata

Author(s): Wilkinson DJ, Arques MdC, Huesa C, Rowan AD

Publication type: Article

Publication status: Published

Journal: British Journal of Pharmacology

Year: 2018

Volume: 176

Issue: 1

Pages: 38-51

Print publication date: 01/01/2019

Online publication date: 23/02/2018

Acceptance date: 09/02/2018

ISSN (print): 0007-1188

ISSN (electronic): 1476-5381

Publisher: John Wiley and Sons Inc.


DOI: 10.1111/bph.14173


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