ArticleChemMedChem2014
Inhibition of cathepsin activity in a cell-based assay by a light-activated ruthenium compound.
Article in ChemMedChem, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 26 papers.
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Who cites it
26 citing papers in PubMed, 63 citations in OpenAlex.
- Ruthenium Complexes in Protein Science: Heading a New Generation of Therapeutic and Analytical Tools.Angewandte Chemie (International ed. in English) · 2026Review
- Mixed Ru(II)-Ir(III) Complexes as Photoactive Inhibitors of the Major Human Drug Metabolizing Enzyme CYP3A4.Inorganic chemistry · 2024Article
- Ruthenium-Based Photoactivated Chemotherapy.Journal of the American Chemical Society · 2023Review
- Metalloimmunotherapy with Rhodium and Ruthenium Complexes: Targeting Tumor-Associated Macrophages.Chemistry (Weinheim an der Bergstrasse, Germany) · 2022Article
- Trifluoromethyl substitution enhances photoinduced activity against breast cancer cells but reduces ligand exchange in Ru(ii) complex.Chemical science · 2021Article
- Photosensitive Ru(II) Complexes as Inhibitors of the Major Human Drug Metabolizing Enzyme CYP3A4.Journal of the American Chemical Society · 2021Article
- Dual-Action Ru(II) Complexes with Bulky π-Expansive Ligands: Phototoxicity without DNA Intercalation.Inorganic chemistry · 2020Article
- New Designs for Phototherapeutic Transition Metal Complexes.Angewandte Chemie (International ed. in English) · 2020Review
- Organoruthenated Nitroxoline Derivatives Impair Tumor Cell Invasion through Inhibition of Cathepsin B Activity.Inorganic chemistry · 2019Article
- Designing Photolabile Ruthenium Polypyridyl Crosslinkers for Hydrogel Formation and Multiplexed, Visible-light Degradation.RSC advances · 2019Article
- Catch and Release Photosensitizers: Combining Dual-Action Ruthenium Complexes with Protease Inactivation for Targeting Invasive Cancers.Journal of the American Chemical Society · 2018Article
- New Ru(ii) complex for dual photochemotherapy: release of cathepsin K inhibitor andDalton transactions (Cambridge, England : 2003) · 2018Article
- Ru(II) Polypyridyl Complexes Derived from Tetradentate Ancillary Ligands for Effective Photocaging.Accounts of chemical research · 2018Article
- Photoactivation of imatinib-antibody conjugate using low-energy visible light from Ru(ii)-polypyridyl cages.Chemical communications (Cambridge, England) · 2018Article
- Ru(ii) polypyridyl complexes as photocages for bioactive compounds containing nitriles and aromatic heterocycles.Chemical communications (Cambridge, England) · 2018Article
- DFT Investigation of Ligand Photodissociation in [RuInorganic chemistry · 2018Article
- A Red-Light-Activated Ruthenium-Caged NAMPT Inhibitor Remains Phototoxic in Hypoxic Cancer Cells.Angewandte Chemie (International ed. in English) · 2017Article
- To cage or to be caged? The cytotoxic species in ruthenium-based photoactivated chemotherapy is not always the metal.Chemical communications (Cambridge, England) · 2017Article
- An Overview Of Photosubstitution Reactions Of Ru(II) Imine Complexes And Their Application In Photobiology And Photodynamic Therapy.Inorganica chimica acta · 2017Article
- Chemical Swarming: Depending on Concentration, an Amphiphilic Ruthenium Polypyridyl Complex Induces Cell Death via Two Different Mechanisms.Chemistry (Weinheim an der Bergstrasse, Germany) · 2016Article
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Authors and funding
9 authors at 3 institutions in 1 country.
Funding
Abstract
Light-activated inhibition of cathepsin activity was demonstrated in a cell-based assay. Inhibitors of cathepsin K, Cbz-Leu-NHCH2 CN (2) and Cbz-Leu-Ser(OBn)-CN (3), were caged within the complexes cis-[Ru(bpy)2 (2)2 ]Cl2 (4) and cis-[Ru(bpy)2 (3)2 ](BF4 )2 (5) (bpy=2,2'-bipyridine) as 1:1 mixtures of Δ and Λ stereoisomers. Complexes 4 and 5 were characterized by (1) H NMR, IR, and UV/Vis spectroscopies and electrospray mass spectrometry. Photochemical experiments confirm that 4 releases two molecules of 2 upon exposure to visible light for 15 min, whereas release of 3 by 5 requires longer irradiation times. IC50 determinations against purified cathepsin K under light and dark conditions with 4 and 5 confirm that inhibition is enhanced from 35- to 88-fold, respectively, upon irradiation with visible light. No apparent toxicity was observed for 4 in the absence or presence of irradiation in bone marrow macrophage (BMM) or PC3 cells, as determined by MTT assays, at concentrations up to 10 μM. Compound 5 is well tolerated at lower concentrations (<1 μM), but does show growth-inhibitory effects at higher concentrations. Confocal microscopy experiments show that 4 decreases intracellular cathepsin activity in osteoclasts with light activation. These results support the further development of caged nitrile-based inhibitors as chemical tools for investigating spatial aspects of proteolysis within living systems.
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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.