5-imino-1, 2, 4-thiadiazoles: first small molecules as substrate competitive inhibitors of glycogen synthase kinase 3

…, S Alonso-Gil, A Encinas, A Castro…

Index: Castro, Ana; Encinas, Arantxa; Gil, Carmen; Braese, Stefan; Porcal, Williams; Perez, Concepcion; Moreno, Francisco J.; Martinez, Ana Bioorganic and Medicinal Chemistry, 2008 , vol. 16, # 1 p. 495 - 510

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Citation Number: 38

Abstract

Cumulative evidence strongly supports that glycogen synthase kinase-3 (GSK-3) is a pathogenic molecule when it is up-dysregulated, emerging as an important therapeutic target in severe unmet human diseases. GSK-3 specific inhibitors might be promising effective drugs for the treatment of devastating pathologies such as neurodegenerative diseases, stroke, and mood disorders. As GSK-3 has the ability to phosphorylate primed ...