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• W2078984524 abstract "The major components of the cartilage extracellular matrix are type II collagen and aggrecan. Type II collagen provides cartilage with its tensile strength, whereas the water-binding capacity of aggrecan provides compressibility and elasticity. Aggrecan breakdown leads to an increase in proteolytic susceptibility of articular collagen; hence, aggrecan may also have a protective effect on type II collagen. Given their role in aggrecan degradation and differing substrate specificity profiles, the pursuit of inhibitors for both aggrecanase 1 (a disintegrin and metalloproteinase with thrombospondin motifs-4 [ADAMTS-4]) and aggrecanase 2 (ADAMTS-5) is desirable. We previously described collagen model fluorescence resonance energy transfer (FRET) substrates for aggrecan-degrading members of the ADAMTS family. These FRET substrate assays are also fully compatible with multiwell formats. In the current study, a collagen model FRET substrate was examined for inhibitor screening of ADAMTS-4. ADAMTS-4 was screened against a small compound library (n = 960) with known pharmacological activity. Five compounds that inhibited ADAMTS-4 > 60% at a concentration of 1 μM were identified. A secondary screen using reversed-phase high-performance liquid chromatography (RP–HPLC) was developed and performed for verification of the five potential inhibitors. Ultimately, piceatannol was confirmed as a novel inhibitor of ADAMTS-4, with an IC50 value of 1 μM. Because the collagen model FRET substrates have distinct conformational features that may interact with protease secondary substrate sites (exosites), nonactive site-binding inhibitors can be identified via this approach. Selective inhibitors for ADAMTS-4 would allow a more definitive evaluation of this protease in osteoarthritis and also represent a potential next generation in metalloproteinase therapeutics." @default.
• W2078984524 created "2016-06-24" @default.
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• W2078984524 date "2008-02-01" @default.
• W2078984524 modified "2023-09-26" @default.
• W2078984524 title "Screening of potential a disintegrin and metalloproteinase with thrombospondin motifs-4 inhibitors using a collagen model fluorescence resonance energy transfer substrate" @default.
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• W2078984524 doi "https://doi.org/10.1016/j.ab.2007.09.014" @default.
• W2078984524 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/2245870" @default.
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