[HTML][HTML] Translational development of an ADAMTS-5 antibody for osteoarthritis disease modification

J Larkin, TA Lohr, L Elefante, J Shearin, R Matico… - Osteoarthritis and …, 2015 - Elsevier
Summary Objective/Method Aggrecanase activity, most notably ADAMTS-5, is implicated in
pathogenic cartilage degradation. Selective monoclonal antibodies (mAbs) to both ADAMTS …

[HTML][HTML] Targeting of ADAMTS5's ancillary domain with the recombinant mAb CRB0017 ameliorates disease progression in a spontaneous murine model of …

R Chiusaroli, M Visentini, C Galimberti… - Osteoarthritis and …, 2013 - Elsevier
Summary Objective ADAMTS5 (aggrecanase-2) has been demonstrated to be crucial in the
development of osteoarthritis (OA), by use of several mouse mutants carrying either …

Anti-ADAMTS5 monoclonal antibodies: implications for aggrecanase inhibition in osteoarthritis

SS Apte - Biochemical Journal, 2016 - portlandpress.com
The extracellular matrix of articular cartilage is structurally specialized for efficient absorption
of mechanical impact. In particular, giant aggregates of the large chondroitin sulfate …

ADAMTS‐4 and ADAMTS‐5: key enzymes in osteoarthritis

P Verma, K Dalal - Journal of cellular biochemistry, 2011 - Wiley Online Library
Osteoarthritis (OA) is a progressive disease of the joints characterized by degradation of
articular cartilage. Although disease initiation may be multi‐factorial, the cartilage …

ADAMTS‐1–knockout mice do not exhibit abnormalities in aggrecan turnover in vitro or in vivo

CB Little, L Mittaz, D Belluoccio… - Arthritis & …, 2005 - Wiley Online Library
Objective To determine the role of the proteinase ADAMTS‐1 in normal and accelerated
catabolism of aggrecan in articular and growth plate cartilage of mice. Methods Expression …

Aggrecan degradation in human articular cartilage explants is mediated by both ADAMTS‐4 and ADAMTS‐5

RH Song, M D. Tortorella, AM Malfait… - … : Official Journal of …, 2007 - Wiley Online Library
Objective Recent published studies have shown that cartilage from ADAMTS‐5–knockout
mice, but not ADAMTS‐4–or ADAMTS‐1–knockout mice, is significantly protected from …

[HTML][HTML] Pharmacological characterization of GLPG1972/S201086, a potent and selective small-molecule inhibitor of ADAMTS5

P Clement-Lacroix, CB Little, MM Smith… - Osteoarthritis and …, 2022 - Elsevier
Objective A disintegrin and metalloproteinase with thrombospondin motifs 5 (ADAMTS5) is a
key enzyme in degradation of cartilage in osteoarthritis (OA). We report the pharmacological …

Characterization of and osteoarthritis susceptibility in ADAMTS‐4–knockout mice

SS Glasson, R Askew, B Sheppard… - … : Official Journal of …, 2004 - Wiley Online Library
Objective To determine the importance of the enzymatic activity of ADAMTS‐4 in normal
growth and development and to evaluate the role of ADAMTS‐4 in the progression of …

Discovery of GLPG1972/S201086, a potent, selective, and orally bioavailable ADAMTS-5 inhibitor for the treatment of osteoarthritis

F Brebion, R Gosmini, P Deprez, M Varin… - Journal of Medicinal …, 2021 - ACS Publications
There are currently no approved disease-modifying osteoarthritis (OA) drugs (DMOADs).
The aggrecanase ADAMTS-5 is key in the degradation of human aggrecan (AGC), a …

[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 …