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

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...

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Main Authors: Chen, W., Gaisina, I., Gunosewoyo, Hendra, Malekiani, S., Hanania, T., Kozikowski, A.
Format: Journal Article
Published: Wiley-VCH Verlag GmbH & Co. KGaA 2011
Subjects:
Online Access:http://hdl.handle.net/20.500.11937/15540
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author Chen, W.
Gaisina, I.
Gunosewoyo, Hendra
Malekiani, S.
Hanania, T.
Kozikowski, A.
author_facet Chen, W.
Gaisina, I.
Gunosewoyo, Hendra
Malekiani, S.
Hanania, T.
Kozikowski, A.
author_sort Chen, W.
building Curtin Institutional Repository
collection Online Access
description 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.
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format Journal Article
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institution Curtin University Malaysia
institution_category Local University
last_indexed 2025-11-14T07:12:42Z
publishDate 2011
publisher Wiley-VCH Verlag GmbH & Co. KGaA
recordtype eprints
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spelling curtin-20.500.11937-155402018-03-29T09:07:21Z Structure-Guided Design of a Highly Selective Glycogen Synthase Kinase-3ß Inhibitor: A Superior Neuroprotective Pyrazolone Showing Antimania Effects Chen, W. Gaisina, I. Gunosewoyo, Hendra Malekiani, S. Hanania, T. Kozikowski, A. kinase selectivity mania GSK-3 neuroprotection bipolar disorders 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. 2011 Journal Article http://hdl.handle.net/20.500.11937/15540 10.1002/cmdc.201100231 Wiley-VCH Verlag GmbH & Co. KGaA restricted
spellingShingle kinase selectivity
mania
GSK-3
neuroprotection
bipolar disorders
Chen, W.
Gaisina, I.
Gunosewoyo, Hendra
Malekiani, S.
Hanania, T.
Kozikowski, A.
Structure-Guided Design of a Highly Selective Glycogen Synthase Kinase-3ß Inhibitor: A Superior Neuroprotective Pyrazolone Showing Antimania Effects
title Structure-Guided Design of a Highly Selective Glycogen Synthase Kinase-3ß Inhibitor: A Superior Neuroprotective Pyrazolone Showing Antimania Effects
title_full Structure-Guided Design of a Highly Selective Glycogen Synthase Kinase-3ß Inhibitor: A Superior Neuroprotective Pyrazolone Showing Antimania Effects
title_fullStr Structure-Guided Design of a Highly Selective Glycogen Synthase Kinase-3ß Inhibitor: A Superior Neuroprotective Pyrazolone Showing Antimania Effects
title_full_unstemmed Structure-Guided Design of a Highly Selective Glycogen Synthase Kinase-3ß Inhibitor: A Superior Neuroprotective Pyrazolone Showing Antimania Effects
title_short Structure-Guided Design of a Highly Selective Glycogen Synthase Kinase-3ß Inhibitor: A Superior Neuroprotective Pyrazolone Showing Antimania Effects
title_sort structure-guided design of a highly selective glycogen synthase kinase-3ß inhibitor: a superior neuroprotective pyrazolone showing antimania effects
topic kinase selectivity
mania
GSK-3
neuroprotection
bipolar disorders
url http://hdl.handle.net/20.500.11937/15540