ArticleBritish journal of pharmacology2018
Tanshinones that selectively block the collagenase activity of cathepsin K provide a novel class of ectosteric antiresorptive agents for bone.
Article in British journal of pharmacology, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 papers.
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Who cites it
18 citing papers in PubMed, 32 citations in OpenAlex.
- Exploration of tropocollagen unwinding by cathepsin K dimer with chondroitin 4-sulphate through microsecond timescale molecular dynamics.Journal of enzyme inhibition and medicinal chemistry · 2026Article
- Local Sodium Tanshinone IIA Sulfonate Attenuates Periodontal Bone Loss by Modulating Inflammatory, Immune and Osteoclastogenic Signalling.Journal of clinical periodontology · 2026Article
- Proteolysis at the extracellular matrix interface: Molecular architects and regulators in health and disease.The FEBS journal · 2026Review
- Integrated machine learning-based virtual screening and biological evaluation for identification of potential inhibitors against cathepsin K.Molecular diversity · 2025Article
- Cathepsin K inhibitors promote osteoclast-osteoblast communication and engagement of osteogenesis.JBMR plus · 2025Article
- Therapeutic Potential of Tanshinones in Osteolytic Diseases: From Molecular and Cellular Pathways to Preclinical Models.Dentistry journal · 2025Review
- Proteins and DNA Sequences Interacting with Tanshinones and Tanshinone Derivatives.International journal of molecular sciences · 2025Review
- Pharmacological impacts of tanshinone on osteogenesis and osteoclastogenesis: a review.Naunyn-Schmiedeberg's archives of pharmacology · 2025Review
- Mechanistic Insights and Therapeutic Strategies in Osteoporosis: A Comprehensive Review.Biomedicines · 2024Review
- scRank infers drug-responsive cell types from untreated scRNA-seq data using a target-perturbed gene regulatory network.Cell reports. Medicine · 2024Article
- Real-time analysis of osteoclast resorption and fusion dynamics in response to bone resorption inhibitors.Scientific reports · 2024Article
- Salvia miltiorrhiza in osteoporosis: a review of its phytochemistry, traditional clinical uses and preclinical studies (2014-2024).Frontiers in pharmacology · 2024Review
- Regulation of Peptidase Activity beyond the Active Site in Human Health and Disease.International journal of molecular sciences · 2023Review
- Article
- Puerarin specifically disrupts osteoclast activation via blocking integrin-β3 Pyk2/Src/Cbl signaling pathway.Journal of orthopaedic translation · 2022Article
- Osteoclasts' Ability to Generate Trenches Rather Than Pits Depends on High Levels of Active Cathepsin K and Efficient Clearance of Resorption Products.International journal of molecular sciences · 2020Article
- The Attenuation of Traumatic Brain Injury via Inhibition of Oxidative Stress and Apoptosis by Tanshinone IIA.Oxidative medicine and cellular longevity · 2020Article
- Tanshinones that selectively block the collagenase activity of cathepsin K provide a novel class of ectosteric antiresorptive agents for bone.British journal of pharmacology · 2018Article
Corrections and comments
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Authors and funding
7 authors at 1 institution in 2 countries.
Funding
Abstract
background and purposeAttempts to generate active site-directed cathepsin K (CatK) inhibitors for the treatment of osteoporosis have failed because of side effects. We have previously shown that an ectosteric tanshinone CatK inhibitor isolated from Salvia miltiorrhiza blocked, selectively, the collagenase activity of CatK, without affecting the active site and demonstrated its bone-preserving activity in vivo. Here, we have characterize the antiresorptive potential of other tanshinones, which may provide a scaffold for side effect-free CatK inhibitors. EXPERIMENTAL APPROACH: Thirty-one tanshinones were tested for their activity against CatK in enzymic and cell-based assays. The inhibitory potency against triple helical and fibrillar collagen degradation was determined in enzymic assays, by scanning electron microscopy and mechanical strength measurements. Human osteoclast assays were used to determine the effects of the inhibitors on bone resorption, its reversibility and osteoclastogenesis. Binding sites were characterized by molecular docking. KEY
resultsTwelve compounds showed highly effective anti-collagenase activity and protected collagen against destruction and mechanical instability without inhibiting the hydrolysis of non-collagenous substrates. Six compounds were highly effective in osteoclast bone resorption assays with IC CONCLUSIONS AND IMPLICATIONS: Our study identified several potent ectosteric antiresorptive CatK inhibitors from the medicinal plant, S. miltiorrhiza, which may avoid side effects seen with active site-directed inhibitors in clinical trials.
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Registered trials
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