arp-100 and Osteoarthritis

arp-100 has been researched along with Osteoarthritis* in 1 studies

Other Studies

1 other study(ies) available for arp-100 and Osteoarthritis

ArticleYear
N-O-isopropyl sulfonamido-based hydroxamates: design, synthesis and biological evaluation of selective matrix metalloproteinase-13 inhibitors as potential therapeutic agents for osteoarthritis.
    Journal of medicinal chemistry, 2009, Aug-13, Volume: 52, Issue:15

    Matrix metalloproteinase-13 (MMP-13) is a key enzyme implicated in the degradation of the extracellular matrix in osteoarthritis (OA). For this reason, MMP-13 synthetic inhibitors are being sought as potential therapeutic agents to prevent cartilage degradation and to halt the progression of OA. Herein, we report the synthesis and in vitro evaluation of a new series of selective MMP-13 inhibitors possessing an arylsulfonamidic scaffold. Among these potential inhibitors, a very promising compound was discovered exhibiting nanomolar activity for MMP-13 and was highly selective for this enzyme compared to MMP-1, -14, and TACE. This compound acted as a slow-binding inhibitor of MMP-13 and was demonstrated to be effective in an in vitro collagen assay and in a model of cartilage degradation. Furthermore, a docking study was conducted for this compound in order to investigate its binding interactions with MMP-13 and the reasons for its selectivity toward MMP-13 versus other MMPs.

    Topics: ADAM Proteins; ADAM17 Protein; Cartilage; Drug Design; Hydroxamic Acids; Matrix Metalloproteinase 1; Matrix Metalloproteinase 13; Matrix Metalloproteinase 14; Matrix Metalloproteinase Inhibitors; Models, Molecular; Osteoarthritis; Protease Inhibitors; Structure-Activity Relationship

2009