Synthesis of novel chemical probes for the study of tanshinone binding proteins.
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.
Lee
Jin-Soo
JS
Laboratory of Chemical Genomics, Bio-Organic Science Division, Korea Research Institute of Chemical Technology, Deajeon 305-600, Republic of Korea.
Han
Sun-Young
SY
Kim
Myong Sang
MS
Yu
Chan-Mo
CM
Kim
Myung Hee
MH
Kim
Seong Hwan
SH
Min
Yong Ki
YK
Kim
Bum Tae
BT
D045784:Abietanes; D000135:Acid Phosphatase / Q000378:metabolism; D000818:Animals; D002352:Carrier Proteins / Q000494:pharmacology; D002460:Cell Line; D049109:Cell Proliferation / Q000187:drug effects; D006859:Hydrogen / Q000737:chemistry; D007527:Isoenzymes / Q000378:metabolism; D008562:Membrane Glycoproteins / Q000494:pharmacology; D051379:Mice; D015394:Molecular Structure; D010010:Osteoclasts / Q000187:drug effects / Q000378:metabolism; D010012:Osteogenesis / Q000187:drug effects; D010616:Phenanthrenes / Q000737:chemistry* / Q000494:pharmacology; D011506:Proteins / Q000737:chemistry*; D053245:RANK Ligand; D053246:Receptor Activator of Nuclear Factor-kappa B; D000071681:Tartrate-Resistant Acid Phosphatase
D045784:Abietanes; D002352:Carrier Proteins; D007527:Isoenzymes; D008562:Membrane Glycoproteins; D010616:Phenanthrenes; D011506:Proteins; D053245:RANK Ligand; D053246:Receptor Activator of Nuclear Factor-kappa B; C505687:Tnfrsf11a protein, mouse; C505689:Tnfsf11 protein, mouse; C021751:tanshinone; D006859:Hydrogen; D000135:Acid Phosphatase; C000605511:Acp5 protein, mouse; D000071681:Tartrate-Resistant Acid Phosphatase