Abstract
Novel diazirine or biotin-labeled tanshinone probes were synthesized and evaluated for TRAP inhibitory activity against RANKL-induced osteoclastogenesis in RAW264.7 cells. We found that diazirine-labeled derivatives (18 and 20) are potent inhibitors of RANKL-induced osteoclastogenesis. IC50 values were 18.02 and 15.00 microM, respectively. These probes will be useful reagents for investigating tanshinone-proteins interactions.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Abietanes
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Acid Phosphatase / metabolism
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Animals
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Carrier Proteins / pharmacology
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Cell Line
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Cell Proliferation / drug effects
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Hydrogen / chemistry
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Isoenzymes / metabolism
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Membrane Glycoproteins / pharmacology
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Mice
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Molecular Structure
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Osteoclasts / drug effects
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Osteoclasts / metabolism
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Osteogenesis / drug effects
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Phenanthrenes / chemistry*
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Phenanthrenes / pharmacology
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Proteins / chemistry*
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RANK Ligand
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Receptor Activator of Nuclear Factor-kappa B
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Tartrate-Resistant Acid Phosphatase
Substances
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Abietanes
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Carrier Proteins
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Isoenzymes
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Membrane Glycoproteins
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Phenanthrenes
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Proteins
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RANK Ligand
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Receptor Activator of Nuclear Factor-kappa B
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Tnfrsf11a protein, mouse
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Tnfsf11 protein, mouse
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tanshinone
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Hydrogen
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Acid Phosphatase
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Acp5 protein, mouse
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Tartrate-Resistant Acid Phosphatase