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 …
osteoarthritis. To identify selective inhibitors of ADAMTS-5, we employed encoded library …
Discovery of potent and selective inhibitors for ADAMTS-4 through DNA-encoded library technology (ELT)
Y Ding, H O'Keefe, JL DeLorey, DI Israel… - ACS Medicinal …, 2015 - ACS Publications
The aggrecan degrading metalloprotease ADAMTS-4 has been identified as a novel
therapeutic target for osteoarthritis. Here, we use DNA-encoded Library Technology (ELT) to …
therapeutic target for osteoarthritis. Here, we use DNA-encoded Library Technology (ELT) to …
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 …
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
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 …
key enzyme in degradation of cartilage in osteoarthritis (OA). We report the pharmacological …
[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 …
pathogenic cartilage degradation. Selective monoclonal antibodies (mAbs) to both ADAMTS …
[HTML][HTML] ADAMTS and ADAM metalloproteinases in osteoarthritis–looking beyond the 'usual suspects'
CY Yang, A Chanalaris, L Troeberg - Osteoarthritis and cartilage, 2017 - Elsevier
Summary Introduction Matrix metalloproteinases (MMPs) and 'aggrecanase'a disintegrin
and metalloproteinase with thrombospondin motifs (ADAMTSs) are well established to play …
and metalloproteinase with thrombospondin motifs (ADAMTSs) are well established to play …
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 …
catabolism of aggrecan in articular and growth plate cartilage of mice. Methods Expression …
ADAMTS5 in osteoarthritis: biological functions, regulatory network, and potential targeting therapies
L Jiang, J Lin, S Zhao, J Wu, Y Jin, L Yu… - Frontiers in molecular …, 2021 - frontiersin.org
ADAMTS5 is involved in the pathogenesis of OA. As the major aggrecanase-degrading
articular cartilage matrix, ADAMTS5, has been regarded as a potential target for OA …
articular cartilage matrix, ADAMTS5, has been regarded as a potential target for OA …
ADAMTS‐9 is synergistically induced by interleukin‐1β and tumor necrosis factor α in OUMS‐27 chondrosarcoma cells and in human chondrocytes
Objective To compare induction of the aggrecanases (ADAMTS‐1, ADAMTS‐4, ADAMTS‐5,
ADAMTS‐8, ADAMTS‐9, and ADAMTS‐15) by interleukin‐1β (IL‐1β) and tumor necrosis …
ADAMTS‐8, ADAMTS‐9, and ADAMTS‐15) by interleukin‐1β (IL‐1β) and tumor necrosis …
The amelioration of cartilage degeneration by ADAMTS-5 inhibitor delivered in a hyaluronic acid hydrogel
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 …
The aggrecanase ADAMTS-5 has been identified as the major enzyme responsible for the …