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

Abstract

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.