Remodelin

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. Remodelin inhibits the growth of prostate cancer and hepatocellular carcinoma in xenograft model. Remodelin enhances the healthspan in hutchinson-gilford progeria syndrome (HGPS) mouse model[1][2][3][4].

[1]Larrieu D, et al. Chemical inhibition of NAT10 corrects defects of laminopathic cells. Science. 2014 May 2;344(6183):527-32.|[2]Ma N, et.al. Inhibition of N-Acetyltransferase 10 Suppresses the Progression of Prostate Cancer through Regulation of DNA Replication. Int J Mol Sci. 2022 Jun 12;23(12):6573. |[3]Balmus G, et.al. Targeting of NAT10 enhances healthspan in a mouse model of human accelerated aging syndrome. Nat Commun. 2018 Apr 27;9(1):1700. |[4]Zhang X, et.al. N-Acetyltransferase 10 Enhances Doxorubicin Resistance in Human Hepatocellular Carcinoma Cell Lines by Promoting the Epithelial-to-Mesenchymal Transition. Oxid Med Cell Longev. 2019 Jul 1;2019:7561879. bioRxiv. 2023 Feb 11.|Cell Death Dis. 2023 Nov 1;14(11):712.|Cell Rep. 2023 Jul 17;42(7):112810.|J Agric Food Chem. 2021 Dec 23.|J Virol. 2024 Jan 3:e0135023.|Life Sci. 2023 Jul 17;121948.|Acta Pharmacol Sin. 2023 Jun 5.|Epigenetics. 2024 Dec;19(1):2417158.|Heliyon. 2023 Jun 8.|J Mol Med (Berl). 2019 Aug;97(8):1183-1193.|Oncogene. 2021 Apr;40(15):2711-2724.