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Pubmed ID :15317461
Publication Date : //

Identification of 1,5-naphthyridine derivatives as a novel series of potent and selective TGF-beta type I receptor inhibitors.


Optimization of the screening hit 1 led to the identification of novel 1,5-naphthyridine aminothiazole and pyrazole derivatives, which are potent and selective inhibitors of the transforming growth factor-beta type I receptor, ALK5. Compounds 15 and 19, which inhibited ALK5 autophosphorylation with IC50 = 6 and 4 nM, respectively, showed potent activities in both binding and cellular assays and exhibited selectivity over p38 mitogen-activated protein kinase. The X-ray crystal structure of 19 in complex with human ALK5 is described, confirming the binding mode proposed from docking studies.

Authors : Gellibert Françoise , Woolven James , Fouchet Marie-Hélène , Mathews Neil , Goodland Helen , Lovegrove Victoria , Laroze Alain , Nguyen Van-Loc , Sautet Stéphane , Wang Ruolan , Janson Cheryl , Smith Ward , Krysa Gaël , Boullay Valérie , De Gouville Anne-Charlotte , Huet Stéphane , Hartley David ,

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