Nicousamide, a potent inhibitor of phosphorylation by TGF-β receptor II

作者:Hai-jing Zhang; Jing Jin; Wan-qi Zhou; Yi Zhang; Yan Li; Jian-yi Liu; Sen Zhang; Xiao-guang Chen
来源:Acta Pharmaceutica Sinica B, 2011, 1(3): 160-165.
DOI:10.1016/j.apsb.2011.05.001

摘要


Renal fibrogenesis is related to the development of diabetic nephropathy. TGF-β receptor II (TGF-β RII) plays a vital role during renal fibrogenesis by phosphorylation and activation of type I receptors and downstream regulators. Nicousamide is a 1.1 class of drug, which can inhibit renal fibrosis in animal models of diabetic nephropathy. After cloning and purification of TGF-β RII, an in vitro substrate phosphorylation assay was set up to investigate the ability of nicousamide to inhibit phosphorylation and formation of cellular downstream proteins. Our results validate nicousamide as a potent inhibitor of phosphorylation of TGF-β RII.