新科学想法 › 文献管理 › 浏览文献

Luteolin inhibition of V-ATPase a3-d2 interaction decreases osteoclast resorptive activity

dr.qinan 添加于 2012-12-8 09:21 | 2284 次阅读 | 0 个评论

作者
Crasto GJ, Kartner N, Yao Y, Li K, Bullock L, Datti A, Manolson MF
摘要
V-ATPase-mediated acid secretion is required for osteoclast bone resorption. Osteoclasts are enriched in V-ATPase a3 and d2 subunit isoforms, and disruption of either of their genes impairs bone resorption. Using purified fusion proteins of a3 N-terminal domain (NTa3) and full-length d subunits we determined in a solid-phase binding assay that half-maximal binding of d1 or d2 to immobilized NTa3 occurs at 3.1 +/- 0.4 or 3.6 +/- 0.6 nM, respectively, suggesting equally high-affinity interactions. A high-throughput modification of this assay was then used to screen chemical libraries for a3-d2 interaction inhibitors, and luteolin, a naturally occurring flavonoid, was identified, with half-maximal inhibition at 2.4 +/- 0.9 microM. Luteolin did not significantly affect NIH/3T3 or RAW 264.7 cell viability, nor did it affect cytokine-induced osteoclastogenesis of RAW 264.7 cells or bone marrow mononuclear cells at concentrations
详细资料
- 文献种类:期刊
- 期刊名称: Journal of Cellular Biochemistry
- 期刊缩写: J Cell Biochem
- 期卷页: 2012年
- 地址: Dental Research Institute, Faculty of Dentistry, University of Toronto, Toronto, Ontario M5G 1G6, Canada
- ISBN: 0730-2312
相关链接 DOI URL