The Anti-ADAMTS-5 Nanobody® M6495 Protects Cartilage Degradation Ex Vivo

AS Siebuhr, D Werkmann, AC Bay-Jensen… - International Journal of …, 2020 - mdpi.com
Osteoarthritis (OA) is associated with cartilage breakdown, brought about by ADAMTS-5
mediated aggrecan degradation followed by MMP-derived aggrecan and type II collagen …

The amelioration of cartilage degeneration by ADAMTS-5 inhibitor delivered in a hyaluronic acid hydrogel

P Chen, S Zhu, Y Wang, Q Mu, Y Wu, Q Xia, X Zhang… - Biomaterials, 2014 - Elsevier
Degradation of proteoglycan is the key early event in the development of osteoarthritis (OA).
The aggrecanase ADAMTS-5 has been identified as the major enzyme responsible for the …

[HTML][HTML] Inflammation and joint destruction may be linked to the generation of cartilage metabolites of ADAMTS-5 through activation of toll-like receptors

N Sharma, P Drobinski, A Kayed, Z Chen… - Osteoarthritis and …, 2020 - Elsevier
Objective Links between pain and joint degradation are poorly understood. We investigated
the role of activation of Toll-like receptors (TLR) by cartilage metabolites in initiating and …

Tumor necrosis factor-α induces ADAMTS-4 expression in human osteoarthritis chondrocytes

J Xue, J Wang, Q Liu, A Luo - Molecular medicine …, 2013 - spandidos-publications.com
Tumor necrosis factor (TNF)-α and a disintegrin and metalloproteinase with thrombospondin
motifs 4 (ADAMTS-4) are important in osteoarthritis (OA) cartilage degradation. In the …

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 …

[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 …

ADAMTS-7 forms a positive feedback loop with TNF-α in the pathogenesis of osteoarthritis

Y Lai, X Bai, Y Zhao, Q Tian, B Liu, EA Lin… - Annals of the …, 2014 - ard.bmj.com
Objective To examine the expression of ADAMTS-7 during the progression of osteoarthritis
(OA), defining its role in the pathogenesis of OA, and elucidating the molecular events …

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 …

Discovery of highly potent and selective small molecule ADAMTS-5 inhibitors that inhibit human cartilage degradation via encoded library technology (ELT)

H Deng, H O'Keefe, CP Davie, KE Lind… - Journal of medicinal …, 2012 - ACS Publications
The metalloprotease ADAMTS-5 is considered a potential target for the treatment of
osteoarthritis. To identify selective inhibitors of ADAMTS-5, we employed encoded library …

Natural compounds: potential therapeutics for the inhibition of cartilage matrix degradation in osteoarthritis

OS Ashruf, MY Ansari - Life, 2022 - mdpi.com
Osteoarthritis (OA) is the most common degenerative joint disease characterized by
enzymatic degradation of the cartilage extracellular matrix (ECM) causing joint pain and …