Publications by authors named "Alessandra Marie Encarnacion"
Article Synopsis
- * A novel inhibitor, KCB-F06, was identified through virtual screening, showing promising effects against osteoclastogenesis in both in vitro and in vivo studies.
- * KCB-F06 reduces ROS accumulation and the activity of key signaling pathways, leading to decreased expression of osteoclast-specific proteins, highlighting its potential as a treatment for osteoclast-related bone diseases.
Both cyclopropyl amide and piperazine sulfonamide functional groups are known for their various biological properties used for drug development. Herein, we synthesized nine new derivatives with different substituent groups incorporating these moieties and screened them for their anti-osteoclast differentiation activity. After analyzing the structure-activity relationship (SAR), the inhibitory effect against osteoclastogenesis was determined to be dependent on the lipophilicity of the compound.
View Article and Find Full Text PDFInhibition of LSD1 was proposed as promising and attractive therapies for treating osteoporosis. Here, we synthesized a series of novel TCP-(MP)-Caffeic acid analogs as potential LSD1 inhibitors to assess their inhibitory effects on osteoclastogenesis by using TRAP-staining assay and try to explore the preliminary SAR. Among them, TCP-MP-CA (11a) demonstrated osteoclastic bone loss both in vitro and in vivo, showing a significant improvement in the in vivo effects compared to the LSD1 inhibitor GSK-LSD1.
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- * Researchers developed new homoisoflavonoid (HIF) derivatives to test their effects on reducing osteoclast formation, identifying derivative 5g as the most effective against osteoclast differentiation without affecting bone formation.
- * The study suggests that 5g works by binding to fibroblast growth factor receptor 1 (FGFR1), which inhibits signaling pathways that contribute to osteoclast formation and bone loss, positioning it as a promising treatment option for osteoporosis.