Abstract
Osteoclasts are one of the key therapeutic targets for a variety of orthopedic diseases such as osteoporosis and osteoarthritis. In this study, we synthesized a novel compound N-(3-(cyclohexylcarbamoyl) phenyl)-1H-indole-2- carboxamide (termed as OA-4) and investigated the effects of OA-4 on the differentiation and function of osteoclasts. OA-4 markedly diminished osteoclast differentiation and osteoclast specific gene expression in a dose-dependent manner. In addition, OA-4 dose-dependently suppressed osteoclastic bone resorption. Furthermore, we found OA-4 attenuated RANKL-induced p38 phosphorylation without affecting JNK or NF-κB signaling pathways. Collectively, we synthesized a novel compound OA-4 which can inhibit osteoclast formation and functions via the suppression of p38 signaling pathway.
Keywords: OA-4, osteoclast formation, osteoclastic bone resorption, osteoporosis, P38 signaling pathway.
Current Medicinal Chemistry
Title:OA-4 Inhibits Osteoclast Formation and Bone Resorption via Suppressing RANKL Induced P38 Signaling Pathway
Volume: 21 Issue: 5
Author(s): B. Tian, A. Qin, Z.Y. Shao, T. Jiang, Z.J. Zhai, H.W. Li, T.T. Tang, Q. Jiang, K.R. Dai, M.H. Zheng, Y.P. Yu and Z.A. Zhu
Affiliation:
Keywords: OA-4, osteoclast formation, osteoclastic bone resorption, osteoporosis, P38 signaling pathway.
Abstract: Osteoclasts are one of the key therapeutic targets for a variety of orthopedic diseases such as osteoporosis and osteoarthritis. In this study, we synthesized a novel compound N-(3-(cyclohexylcarbamoyl) phenyl)-1H-indole-2- carboxamide (termed as OA-4) and investigated the effects of OA-4 on the differentiation and function of osteoclasts. OA-4 markedly diminished osteoclast differentiation and osteoclast specific gene expression in a dose-dependent manner. In addition, OA-4 dose-dependently suppressed osteoclastic bone resorption. Furthermore, we found OA-4 attenuated RANKL-induced p38 phosphorylation without affecting JNK or NF-κB signaling pathways. Collectively, we synthesized a novel compound OA-4 which can inhibit osteoclast formation and functions via the suppression of p38 signaling pathway.
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Tian B., Qin A., Shao Z.Y., Jiang T., Zhai Z.J., Li H.W., Tang T.T., Jiang Q., Dai K.R., Zheng M.H., Yu Y.P. and Zhu Z.A., OA-4 Inhibits Osteoclast Formation and Bone Resorption via Suppressing RANKL Induced P38 Signaling Pathway, Current Medicinal Chemistry 2014; 21 (5) . https://dx.doi.org/10.2174/09298673113209990190
DOI https://dx.doi.org/10.2174/09298673113209990190 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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