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.

Keywords

• Nicousamide
• Renal fibrosis
• Phosphorylation
• TGF-β receptor II