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

Autor: Hai-jing Zhang, Jing Jin, Wan-qi Zhou, Yi Zhang, Yan Li, Jian-yi Liu, Sen Zhang, Xiao-guang Chen
Jazyk: angličtina
Rok vydání: 2011
Předmět:
Zdroj: Acta Pharmaceutica Sinica B, Vol 1, Iss 3, Pp 160-165 (2011)
Druh dokumentu: article
ISSN: 2211-3835
2211-3843
DOI: 10.1016/j.apsb.2011.05.001
Popis: 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.
Databáze: Directory of Open Access Journals