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 |
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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 |
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