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Structure-Guided Design of a Highly Selective Glycogen Synthase Kinase-3ß Inhibitor: A Superior Neuroprotective Pyrazolone Showing Antimania Effects

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Chen, W.
Gaisina, I.
Gunosewoyo, Hendra
Malekiani, S.
Hanania, T.
Kozikowski, A.
Date
2011
Type
Journal Article

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Chen, Wenwen and Gaisina, Irina N. and Gunosewoyo, Hendra and Malekiani, Sam A. and Hanania, Taleen and Kozikowski, Alan P. 2011. Structure-Guided Design of a Highly Selective Glycogen Synthase Kinase-3ß Inhibitor: A Superior Neuroprotective Pyrazolone Showing Antimania Effects. ChemMedChem. 6 (9): pp. 1587-1592.
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ChemMedChem
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Abstract

A new craze! A new chemical scaffold, namely a staurosporine-like molecule (shown) possessing a pyrazolone core, was found to be highly selective for glycogen synthase kinase 3 over a group of other homologous kinases, including typical cyclin-dependent kinases. This compound gave an impressive dose–response curve for neuroprotection in the homocysteic acid model of oxidative stress (graph shown), and furthermore, blocked chemically induced mania-like effects in mice.