Document Detail

Novel indolylmaleimide acts as GSK-3beta inhibitor in human neural progenitor cells.
MedLine Citation:
PMID:  20708937     Owner:  NLM     Status:  MEDLINE    
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.
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:
Type:  Journal Article; Research Support, Non-U.S. Gov't     Date:  2010-07-25
Journal Detail:
Title:  Bioorganic & medicinal chemistry     Volume:  18     ISSN:  1464-3391     ISO Abbreviation:  Bioorg. Med. Chem.     Publication Date:  2010 Sep 
Date Detail:
Created Date:  2010-09-06     Completed Date:  2010-12-30     Revised Date:  2011-11-02    
Medline Journal Info:
Nlm Unique ID:  9413298     Medline TA:  Bioorg Med Chem     Country:  England    
Other Details:
Languages:  eng     Pagination:  6785-95     Citation Subset:  IM    
Copyright Information:
Copyright (c) 2010 Elsevier Ltd. All rights reserved.
Albrecht-Kossel-Institute for Neuroregeneration (AKos), Center for Mental Health, University of Rostock, Gehlsheimer Str. 20, D-18147 Rostock, Germany.
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MeSH Terms
Cell Differentiation
Cell Proliferation
Glycogen Synthase Kinase 3 / antagonists & inhibitors*,  metabolism
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
Reg. No./Substance:
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 synthase kinase 3 beta; EC Synthase Kinase 3

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