Targeting aggrecanases for osteoarthritis therapy: from zinc chelation to exosite inhibition
Osteoarthritis (OA) is the most common degenerative joint disease. In 1999, two members of
the A Disintegrin and Metalloproteinase with Thrombospondin Motifs (ADAMTS) family of …
the A Disintegrin and Metalloproteinase with Thrombospondin Motifs (ADAMTS) family of …
Progress towards the identification of new aggrecanase inhibitors
F De Rienzo, P Saxena, F Filomia… - Current medicinal …, 2009 - ingentaconnect.com
Degenerative diseases are still a challenging issue in clinical therapy; even though in
several cases it is possible to treat symptoms, drugs able to block disease progression are …
several cases it is possible to treat symptoms, drugs able to block disease progression are …
Drug insight: aggrecanases as therapeutic targets for osteoarthritis
AJ Fosang, CB Little - Nature clinical practice Rheumatology, 2008 - nature.com
In healthy cartilage, effective weight-bearing requires a high concentration of intact
aggrecan. Degradation and loss of aggrecan are features of osteoarthritis (OA). It is unclear …
aggrecan. Degradation and loss of aggrecan are features of osteoarthritis (OA). It is unclear …
Inhibition of aggrecanases as a therapeutic strategy in osteoarthritis
JE Bakali, H Gras-Masse, L Maingot… - Future Medicinal …, 2014 - Future Science
Over the last decade, there has been a large effort to target aggrecanases, which are
responsible for the degradation of the aggrecan in the extracellular matrix of joints, in order …
responsible for the degradation of the aggrecan in the extracellular matrix of joints, in order …
Antibody-based exosite inhibitors of ADAMTS-5 (aggrecanase-2)
S Santamaria, K Yamamoto, K Botkjaer… - Biochemical …, 2015 - portlandpress.com
Adamalysin-like metalloproteinases with thrombospondin (TS) motifs (ADAMTS)-5 is the
multi-domain metalloproteinase that most potently degrades aggrecan proteoglycan in the …
multi-domain metalloproteinase that most potently degrades aggrecan proteoglycan in the …
GLPG1972: a potent, selective, orally available adamts-5 inhibitor for the treatment of OA
P Clement-Lacroix, C Little, S Meurisse… - Osteoarthritis and …, 2017 - oarsijournal.com
Purpose: Increased aggrecanase activity is a well-known trigger factor for osteoarthritis (OA),
initiating loss of cartilage aggrecan that precedes more severe cartilage degradation. A …
initiating loss of cartilage aggrecan that precedes more severe cartilage degradation. A …
Identification of potent and selective hydantoin inhibitors of aggrecanase-1 and aggrecanase-2 that are efficacious in both chemical and surgical models of …
TB Durham, VJ Klimkowski, CJ Rito… - Journal of Medicinal …, 2014 - ACS Publications
A disintegrin and metalloproteinase with thrombospondin motifs-4 (ADAMTS-4) and
ADAMTS-5 are zinc metalloproteases commonly referred to as aggrecanase-1 and …
ADAMTS-5 are zinc metalloproteases commonly referred to as aggrecanase-1 and …
Advances in the development of novel aggrecanase inhibitors
AM Gilbert, JA Bikker, SV O'Neil - Expert Opinion on Therapeutic …, 2011 - Taylor & Francis
Importance of the field: Aggrecanases are members of a disintegrin and metalloprotease
with thrombospondin motif family of zinc metalloproteases involved in the cleavage of …
with thrombospondin motif family of zinc metalloproteases involved in the cleavage of …
[PDF][PDF] The “elusive DMOAD”: Aggrecanase inhibition from laboratory to clinic
AM Malfait, MD Tortorella - Clin. Exp. Rheumatol, 2019 - clinexprheumatol.org
From the time of their discovery in 1999, the aggrecanases, and ADAMTS-5 in particular,
have been heavily investigated as targets for disease-modifying osteoarthritis drug …
have been heavily investigated as targets for disease-modifying osteoarthritis drug …
Will the real aggrecanase (s) step up: evaluating the criteria that define aggrecanase activity in osteoarthritis
MD Tortorella, AM Malfait - Current pharmaceutical …, 2008 - ingentaconnect.com
Loss of aggrecan from articular cartilage is an early and critical event in the pathogenesis of
osteoarthritis (OA) and is enzymatically mediated by aggrecanase activity. Since the …
osteoarthritis (OA) and is enzymatically mediated by aggrecanase activity. Since the …