Results 131 to 140 of about 11,934 (162)
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Characterization of the human ADAMTS-5 (aggrecanase-2) gene promoter
Molecular Biology Reports, 2007Aggrecan 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
Biochimie, 2022
There is a critical need for the development of more potent inhibitors for osteoarthritis (OA) therapy given the poor life quality of arthritis patients. Aggrecanase ADAMTS-5 (a disintegrin and metalloproteinase with thrombospondin motifs 5) is an established drug target identified for osteoarthritis. In this study, we evolved and characterized two new
Yuanyuan Yu +4 more
openaire +2 more sources
There is a critical need for the development of more potent inhibitors for osteoarthritis (OA) therapy given the poor life quality of arthritis patients. Aggrecanase ADAMTS-5 (a disintegrin and metalloproteinase with thrombospondin motifs 5) is an established drug target identified for osteoarthritis. In this study, we evolved and characterized two new
Yuanyuan Yu +4 more
openaire +2 more sources
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
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, 2009Aggrecan 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
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Synthesis and evaluation of aryl thioxothiazolidinone inhibitors of ADAMTS-5 (Aggrecanase-2)
Bioorganic & Medicinal Chemistry Letters, 20075-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
Biomaterials, 2014
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 degradation and thus is an attractive therapeutic target for OA. However, currently there is no report on using an ADAMTS-5 inhibition strategy for OA treatment.
Heng Sun, Yan Wu, Hu Hu
exaly +3 more sources
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 degradation and thus is an attractive therapeutic target for OA. However, currently there is no report on using an ADAMTS-5 inhibition strategy for OA treatment.
Heng Sun, Yan Wu, Hu Hu
exaly +3 more sources
Discovery of a benzimidazole series of ADAMTS-5 (aggrecanase-2) inhibitors by scaffold hopping
European Journal of Medicinal Chemistry, 2014We 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
Inhibition of ADAMTS-5: the right target for osteoarthritis?
Osteoarthritis and Cartilage, 2022A. Latourte, P. Richette
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Impact Of Activating Adamts-5 In Cartilage-related Degenerative Disorders
2010The 2010 World Forum for Spine Research (WFSR 2010): The Intervertebral Disc, Montreal, Canada, 5-8 July 2010.
Fosang, AMANDA +5 more
openaire +4 more sources
Peptide Vaccine Against ADAMTS-7 Ameliorates Atherosclerosis and Postinjury Neointima Hyperplasia
Circulation, 2023Wei Kong, Qingbo Xu, Yiting Jia
exaly