基于靶点的 p300 组蛋白乙酰转移酶抑制剂的合理设计及作为抗纤维化药物的系统评价。
Field-based rational design of p300 histone acetyltransferase inhibitor and systematic evaluation as an anti-fibrotic agent.
机构信息
College of Pharmacy & Graduate School of Pharmaceutical Sciences, Ewha Womans University, Seoul, 03760, Korea.
Department of Biochemistry and Molecular Biology, Severance Medical Research Institute, Brain Korea 21 PLUS Project for Medical Sciences, Yonsei University College of Medicine, Seoul, 03722, Korea.
出版信息
Chem Commun (Camb). 2020 Aug 25;56(68):9795-9798. doi: 10.1039/d0cc03553j.
(E)-3-(3-(4-((3-Carbamoylbenzyl)oxy)-3-iodo-5-methoxyphenyl) acryloyl)benzamide (A6) was found to be a potent p300 inhibitor (IC50 = 870 nM) showing a similar binding mode to that of acetyl-CoA, a p300 substrate, and effective anti-fibrotic activity in both TGF-β1-stimulated lung fibroblast cells and bleomycin-induced in vivo lung fibrosis mice.
（E）-3-（3-（4-（（3-氨甲酰苄基）氧基）-3-碘-5-甲氧基苯基）丙烯酰基）苯甲酰胺（A6）被发现是一种有效的 p300 抑制剂（IC50 = 870 nM），其结合模式与 p300 底物乙酰-CoA 相似，在 TGF-β1 刺激的肺成纤维细胞和博来霉素诱导的体内肺纤维化小鼠中均具有有效的抗纤维化活性。
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