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Open AccessArticle

PSTP-3,5-Me Inhibits Osteoclast Differentiation and Bone Resorption

1
Department of Oral Biochemistry, Dental Science Research Institute, School of Dentistry, Chonnam National University, Gwangju 61186, Korea
2
Department of Molecular Medicine (BK21plus), Chonnam National University Graduate School, Gwangju 61186, Korea
3
Department of Chemistry, Chonnam National University, Gwangju 61186, Korea
*
Author to whom correspondence should be addressed.
Molecules 2019, 24(18), 3346; https://doi.org/10.3390/molecules24183346
Received: 3 September 2019 / Accepted: 12 September 2019 / Published: 14 September 2019
Osteogenesis is an orchestrated process regulated by osteoclastogenesis and osteoblastogenesis. Excessive osteoclastogenesis causes bone diseases, such as osteoporosis. Although a few drugs are effective in osteoporosis treatment, these drugs lead to side effects, including cellulitis, flatulence, and hypocalcemia. In this study, we reported a 2-(N-Phenylmethylsulfonamido)-N-(2-(phenylthio)phenyl)propanamide (PSTP) compound, PSTP-3,5-Me, as a potential therapeutic agent for osteoporosis. Mouse bone marrow-derived macrophages (BMMs) were differentiated into osteoclasts by receptor activator of nuclear factor kappa B ligand (RANKL) and macrophage colony-stimulating factor (M-CSF) in the presence of PSTP-3,5-Me. PSTP-3,5-Me inhibited osteoclast differentiation by reduced tartrate-resistant acid phosphatase (TRAP)-positive osteoclasts, and suppressed the expression of osteoclast marker genes, such as cathepsin K (Ctsk) and TRAP (Acp5). We investigated signaling pathways mediated by RANKL and its receptor, RANK, and found that PSTP-3,5-Me inhibits nucleus translocation of nuclear factor of activated T cell cytoplasmic-1 (NFATc1). Moreover, PSTP-3,5-Me inhibited F-actin ring formation and mineral resorption. Overall, our data suggests that PSTP-3,5-Me attenuates osteoclast differentiation by blocking the activation of NFATc1. View Full-Text
Keywords: osteoclastogenesis; osteoporosis; PSTP; NFATc1 osteoclastogenesis; osteoporosis; PSTP; NFATc1
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Cho, E.; Chen, Z.; Lee, J.; Lee, S.; Lee, T.-H. PSTP-3,5-Me Inhibits Osteoclast Differentiation and Bone Resorption. Molecules 2019, 24, 3346.

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