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ADAMTS-5 inhibition reduces muscle inflammation and fibrosis and improves function in mouse models of Duchenne muscular dystrophy.

Science Translational Medicine
In muscles of patients with Duchenne muscular dystrophy (DMD), expression of extracellular matrix proteases and proteoglycans, including A disintegrin and metalloproteinase with thrombospondin motifs 5 (ADAMTS-5) and its substrates versican and ...
John Dulos   +7 more
semanticscholar   +1 more source

Characterization of the human ADAMTS-5 (aggrecanase-2) gene promoter

Molecular Biology Reports, 2007
Aggrecan degradation in osteoarthritis is mediated primarily by aggrecanases (-1 and -2) that are members of the ADAMTS family of proteases. Aggrecanase-2 (ADAMTS-5) null mice are resistant to aggrecan degradation in models of experimentally-induced osteoarthritis.
Kannan, Thirunavukkarasu   +2 more
openaire   +2 more sources

Decreased histone H3K9 dimethylation in synergy with DNA demethylation of Spi‐1 binding site contributes to ADAMTS‐5 expression in articular cartilage of osteoarthritis mice

Journal of Cellular Physiology
Osteoarthritis (OA) is defined by articular cartilage degeneration, synovial membrane inflammation, and abnormal bone remodeling. Recent study has discovered that OA development is linked to an aberrant epigenetic modification of OA‐related genes.
Shuaichen Yan   +5 more
semanticscholar   +1 more source

AB0047 ACTIVATION OF TLR2 BY ADAMTS-5-MEDIATED DEGRADATION FRAGMENTS OF CARTILAGE EXPLANTS IS INHIBITED BY THE ANTI-ADAMTS-5 NANOBODY®, M6495

Annals of the Rheumatic Diseases, 2019
Background: Patients with joint diseases such as osteoarthritis (OA) are believed to have an abundance of endogenous Toll like receptor (TLR) ligands in their joints, which might be responsible for activating TLRs that may ultimately initiate a self-perpetuating inflammatory loop in the disease.
Neha Sharma   +8 more
openaire   +1 more source

Syndecan-4 regulates ADAMTS-5 activation and cartilage breakdown in osteoarthritis

Nature Medicine, 2009
Aggrecan cleavage by a disintegrin and metalloproteinase with a thrombospondin type 1 motif, member 5 (ADAMTS-5) is crucial for the breakdown of cartilage matrix during osteoarthritis, a degenerative joint disease that leads to the progressive destruction of articular structures. The mechanisms of ADAMTS-5 activation and their links to the pathogenesis
Frank, Echtermeyer   +10 more
openaire   +2 more sources

Synthesis and evaluation of aryl thioxothiazolidinone inhibitors of ADAMTS-5 (Aggrecanase-2)

Bioorganic & Medicinal Chemistry Letters, 2007
5-Benzylidene-2-thioxo-thiazolidin-4-one inhibitors of ADAMTS-5 (Aggrecanase-2) have been prepared via commercially available starting materials. The identified compounds show micromolar ADAMTS-5 potency and demonstrate SAR trends for both the aryl group and thioxothiazolidinone zinc chelator.
Matthew G, Bursavich   +6 more
openaire   +2 more sources

Long non-coding RNA HOTAIR promotes expression of ADAMTS-5 in human osteoarthritic articular chondrocytes.

Pharmazie, 2017
Accumulating evidence indicated that inhibiting the expression of a disintegrin and metalloproteinase with thrombospondin motifs (ADAMTS)-5 ameliorate cartilage degradation, suggesting ADAMTS-5 as an effective target for treating osteoarthritis (OA).
Pengcheng Dou   +6 more
semanticscholar   +1 more source

Expression Levels of A disintegrin-like metalloproteinase with thrombospondin motifs-4 and -5 (ADAMTS-4 and ADAMTS-5) in inflamed and healthy gingival tissues.

Combinatorial chemistry & high throughput screening, 2020
BACKGROUND ADAMTS (A disintegrin-like metalloproteinase with thrombospondin motifs) is a group of 19 zinc-dependent metalloproteases known to function in many pathological and physiological processes, such as adhesion, cell fusion, signaling, proteolysis
M. Tayman   +2 more
semanticscholar   +1 more source

The investigation of serum levels of ADAMTS 5 and 8 (the A disintegrin and metalloproteinase with thrombospondin motifs) in the etiology of endometrial cancer

Journal of Obstetrics and Gynaecology Research, 2019
The aim of this study was to investigate the serum levels of the A disintegrin and metalloproteinase with thrombospondin motifs (ADAMTS) 5 and 8 in patients diagnosed with endometrial cancer.
E. Yılmaz   +4 more
semanticscholar   +1 more source

Discovery of a benzimidazole series of ADAMTS-5 (aggrecanase-2) inhibitors by scaffold hopping

European Journal of Medicinal Chemistry, 2014
We describe a medicinal chemistry approach to generate a series of benzimidazoles bearing thiazolidin-4-one using scaffold hopping from thiazole 1, our previously described thiazole. Our goal was to discover a potent and permeable small-molecule ADAMTS-5 inhibitor.
Shinya Sogame   +5 more
openaire   +2 more sources

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