Remodelin is an orally active and selective inhibitor of acetyltransferase NAT10. Remodelin inhibits NAT10 activitity and slows DNA replication and suppresses growth of prostate cancer cells.Additionally, Remodelin curtails the development of prostate cancer and hepatocellular carcinoma in xenograft models and prolongs the lifespan in models of Hutchinson-Gilford Progeria Syndrome (HGPS)[1].[2].[3].[4].
体外研究
When applied in concentrations ranging from 10 to 40 μΜ over a period of 1 to 7 days, Remodelin systematically diminishes NAT10 activity and cell growth in a concentration-responsive manner across both AR-positive and AR-negative prostate cancer cell types[2].
At a dosage of 20 μΜ for a duration of 24 hours, it specifically reduces NAT10 activity and decelerates DNA synthesis in prostate cancer cells[2].
Moreover, a 7-day treatment with Remodelin at 1 μΜ lessens nuclear abnormalities and bolsters genomic integrity in LmnaG609G/G609G fibroblasts[3].
Intraperitoneal injection (i.p.), once every two days for 4 weeks, Remodelin significantly reduced AR-negative prostate cancer tumor growth in PC-3 cells tumor xenograft model in nude athymic BALB/c nu/nu mice[2].
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