ArticleScientific reports2025
Design, synthesis and biological activity of glycoconjugated ADAMTS5 exosite inhibitors: applications in osteoarthritis and ovarian cancer models.
Article in Scientific reports, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 1 paper.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
1 citing paper in PubMed.
- Current Advances in the Physiological Roles and Disease-Associated Mechanisms of ADAMTS16.International journal of molecular sciences · 2026Review
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
15 authors.
Funding
Abstract
Pharmacological inhibition of the extracellular zinc metalloprotease A Disintegrin-like And Metalloprotease domain with Thrombospondin type I motifs 5 (ADAMTS5) has been proposed as a treatment for osteoarthritis (OA), a degenerative disease characterized by cartilage loss. More recently, ADAMTS5 has been implicated in ovarian cancer (OC), due to its essential role in promoting cell migration and association with poor prognosis. ADAMTS5 major substrates are the proteoglycans aggrecan and versican, which support the structural integrity of the cartilage and the tumor microenvironment. We have recently described a non-chelating arylsulfonamide glycoconjugate, compound 4b, as a selective ADAMTS5 inhibitor, and shown its effectiveness in an OC 3D model. Here, we modified the structure of 4b to improve its biological activity. We showed that, while 4b induces cytotoxicity in several cell lines as well as in porcine and human cartilage explants, its derivative 2 was tolerated at high micromolar concentrations and effective in inhibiting aggrecan degradation in human ex vivo OA explants and reducing directional OC cell migration and pseudopod elongation. In silico analyses provided a rationale behind the different biological activities of the two compounds. These findings highlight the potential of non-chelating glycoconjugated arylsulfonamides to treat pathologies characterized by excessive ADAMTS5 activity.
Indexed as
Identifiers
What OpenQuestion holds
Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.