Abstract
We screened small-molecule compounds that inhibit osteoclast differentiation to find new anti-osteoporosis agents and found that a novel compound, SUKU-1, suppressed osteoclastogenesis. We also synthesized 38 derivatives of SUKU-1 and discovered that nine of them had inhibitory effects on osteoclastogenesis and that SUKU-33 was the most potent inhibitor. Next, we investigated the mechanisms by which SUKU-33 suppressed osteoclast differentiation. By measuring the uptake of [3H]-uridine in cells, we found that SUKU-33 suppressed both equilibrative nucleoside transporters and concentrative nucleoside transporters. These results suggest that SUKU-33 inhibits osteoclast differentiation by suppressing nucleoside transporters.
| Original language | English |
|---|---|
| Pages (from-to) | 1152-1162 |
| Number of pages | 11 |
| Journal | FEBS Letters |
| Volume | 590 |
| Issue number | 8 |
| DOIs | |
| Publication status | Published - 2016 Apr 1 |
Keywords
- concentrative nucleoside transporter
- equilibrative nucleoside transporter
- osteoclast differentiation
- osteoporosis
ASJC Scopus subject areas
- Biophysics
- Structural Biology
- Biochemistry
- Molecular Biology
- Genetics
- Cell Biology
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Cite this
Katsuyama, S., Sugino, K., Sasazawa, Y., Nakano, Y., Aono, H., Morishita, K., Kawatani, M., Umezawa, K., Osada, H., & Simizu, S. (2016). Identification of a novel compound that inhibits osteoclastogenesis by suppressing nucleoside transporters. FEBS Letters, 590(8), 1152-1162. https://doi.org/10.1002/1873-3468.12146