| Novel indolylmaleimide acts as GSK-3beta inhibitor in human neural progenitor cells. | |
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MedLine Citation:
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PMID: 20708937 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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The Wnt pathway is involved in cellular processes linked to either proliferation or differentiation. Therefore small molecules offer an attractive opportunity to modulate this pathway, whereas the key enzyme GSK-3beta is of special interest. In this study, non-symmetrically substituted indolylmaleimides have been synthesized and their ability to function as GSK-3beta inhibitors has been investigated in a human neural progenitor cell line. Among the newly synthesized compounds, the substance IM-12 showed a significant activity in several biological tests which was comparable or even outplayed the effects of the known GSK-3beta inhibitor SB-216763. Furthermore the treatment of human neural progenitor cells with IM-12 resulted in an increase of neuronal cells. Therefore we conclude that indolylmaleimides act via the canonical Wnt signalling pathway by inhibition of the key enzyme GSK-3beta. |
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Authors:
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Anne-Caroline Schmöle; Anne Brennführer; Gnuni Karapetyan; Robert Jaster; Anahit Pews-Davtyan; Rayk Hübner; Stefanie Ortinau; Matthias Beller; Arndt Rolfs; Moritz J Frech |
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Publication Detail:
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Type: Journal Article; Research Support, Non-U.S. Gov't Date: 2010-07-25 |
Journal Detail:
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Title: Bioorganic & medicinal chemistry Volume: 18 ISSN: 1464-3391 ISO Abbreviation: Bioorg. Med. Chem. Publication Date: 2010 Sep |
Date Detail:
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Created Date: 2010-09-06 Completed Date: 2010-12-30 Revised Date: 2011-11-02 |
Medline Journal Info:
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Nlm Unique ID: 9413298 Medline TA: Bioorg Med Chem Country: England |
Other Details:
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Languages: eng Pagination: 6785-95 Citation Subset: IM |
Copyright Information:
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Copyright (c) 2010 Elsevier Ltd. All rights reserved. |
Affiliation:
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Albrecht-Kossel-Institute for Neuroregeneration (AKos), Center for Mental Health, University of Rostock, Gehlsheimer Str. 20, D-18147 Rostock, Germany. |
Export Citation:
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| MeSH Terms | |
Descriptor/Qualifier:
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Cell Differentiation Cell Proliferation Glycogen Synthase Kinase 3 / antagonists & inhibitors*, metabolism Humans Indoles / chemical synthesis, chemistry*, pharmacology Maleimides / chemical synthesis, chemistry*, pharmacology Neurons / cytology* Protein Kinase Inhibitors / chemical synthesis, chemistry*, pharmacology Signal Transduction Stem Cells / cytology, enzymology* Wnt Proteins / metabolism beta Catenin / metabolism |
| Chemical | |
Reg. No./Substance:
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0/3-(4-fluorophenylethylamino)-1-methyl-4-(2-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione; 0/Indoles; 0/Maleimides; 0/Protein Kinase Inhibitors; 0/SB 216763; 0/Wnt Proteins; 0/beta Catenin; 541-59-3/maleimide; EC 2.7.11.1/glycogen synthase kinase 3 beta; EC 2.7.11.26/Glycogen Synthase Kinase 3 |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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