9-Cyano-1-azapaullone (cazpaullone), a glycogen synthase kinase-3 (GSK-3) inhibitor activating pancreatic β cell protection and replication

H Stukenbrock, R Mussmann, M Geese…

Index: Stukenbrock, Hendrik; Mussmann, Rainer; Geese, Marcus; Ferandin, Yoan; Lozach, Olivier; Lemcke, Thomas; Kegel, Simone; Lomow, Alexander; Burk, Ulrike; Dohrmann, Cord; Meijer, Laurent; Austen, Matthias; Kunick, Conrad Journal of Medicinal Chemistry, 2008 , vol. 51, # 7 p. 2196 - 2207

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Citation Number: 62

Abstract

Recently, the serine/threonine kinase glycogen synthase kinase-3 (GSK-3) emerged as a regulator of pancreatic β cell growth and survival. On the basis of the previous observation that GSK-3 inhibitors like 1-azakenpaullone promote β cell protection and replication, paullone derivatives were synthesized including 1-aza-, 2-aza-, and 12-oxapaullone scaffolds. In enzymatic assays distinct 1-azapaullones were found to exhibit selective GSK ...