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5-Lipoxygenase inhibitors suppress RANKL-induced osteoclast formation via NFATc1 expression
- 5-Lipoxygenase inhibitors suppress RANKL-induced osteoclast formation via NFATc1 expression
- Kang, Ju-Hee; Ting, Zheng; Moon, Mi-ran; Sim, Jung-Seon; Lee, Jung-Min; Doh, Kyung-Eun; Hong, Sunhye; Cui, Minghua; Choi, Sun; Chang, Hyeun Wook; Choo, Hea-Young Park; Yim, Mijung
- Ewha Authors
- 박혜영; 최선
- SCOPUS Author ID
- 박혜영; 최선
- Issue Date
- Journal Title
- BIOORGANIC & MEDICINAL CHEMISTRY
- 0968-0896; 1464-3391
- vol. 23, no. 21, pp. 7069 - 7078
- 5-Lipoxygenase; Benzoxazole scaffold; RANKL-induced osteoclast formation; NFATc1; Lipopolysaccharide (LPS)-induced osteoclast formation
- PERGAMON-ELSEVIER SCIENCE LTD
- SCI; SCIE; SCOPUS
- 5-Lipoxygenase synthesizes leukotrienes from arachidonic acid. We developed three novel 5-LO inhibitors having a benzoxazole scaffold as a potential anti-osteoclastogenics. They significantly suppressed RANKL-induced osteoclast formation in mouse bone marrow-derived macrophages. Furthermore, one compound, K7, inhibited the bone resorptive activity of osteoclasts. The anti-osteoclastogenic effect of K7 was mainly attributable to reduction in the expression of NFATc1, an essential transcription factor for osteoclast differentiation. K7 inhibited osteoclast formation via ERR and p38 MAPK, as well as NF-kappa B signaling pathways. K7 reduced lipopolysaccharide (LPS)-induced osteoclast formation in vivo, corroborating the in vitro data. Thus, K7 exerted an inhibitory effect on osteoclast formation in vitro and in vivo, properties that make it a potential candidate for the treatment of bone diseases associated with excessive bone resorption. (C) 2015 Elsevier Ltd. All rights reserved.
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