An aminopyridazine-based inhibitor of a pro-apoptotic protein kinase attenuates hypoxia-ischemia induced acute brain injury

…, M Zasadzki, S Mirzoeva, AM Schumacher…

Index: Velentza, Anastasia V.; Wainwright, Mark S.; Zasadzki, Magdalena; Mirzoeva, Salida; Schumacher, Andrew M.; Haiech, Jacques; Focia, Pamela J.; Egli, Martin; Watterson, D. Martin Bioorganic and Medicinal Chemistry Letters, 2003 , vol. 13, # 20 p. 3465 - 3470

Full Text: HTML

Citation Number: 70

Abstract

Death associated protein kinase (DAPK) is a calcium and calmodulin regulated enzyme that functions early in eukaryotic programmed cell death, or apoptosis. To validate DAPK as a potential drug discovery target for acute brain injury, the first small molecule DAPK inhibitor was synthesized and tested in vivo. A single injection of the aminopyridazine-based inhibitor administered 6 h after injury attenuated brain tissue or neuronal biomarker loss measured, ...