Literature DB >> 14698171

1-Azakenpaullone is a selective inhibitor of glycogen synthase kinase-3 beta.

Conrad Kunick1, Kathrin Lauenroth, Maryse Leost, Laurent Meijer, Thomas Lemcke.   

Abstract

Kenpaullone derivatives with a modified parent ring system were synthesized in order to develop kinase inhibitors with enhanced selectivity. Among the novel structures, 1-azakenpaullone was found to act as a selective GSK-3beta versus CDK1 inhibitor. The charge distribution within the 1-azakenpaullone molecule is discussed as a possible explanation for the enhanced GSK-3beta selectivity of 1-azakenpaullone compared to other paullone derivatives.

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Year:  2004        PMID: 14698171     DOI: 10.1016/j.bmcl.2003.10.062

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  49 in total

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2.  Amphioxus Sp5 is a member of a conserved Specificity Protein complement and is modulated by Wnt/β-catenin signalling.

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3.  Planarian GSK3s are involved in neural regeneration.

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Journal:  Dev Genes Evol       Date:  2008-01-16       Impact factor: 0.900

4.  Parallel synthesis of a series of non-functional ATP/NAD analogs with activity against trypanosomatid parasites.

Authors:  Andreas Link; Philipp Heidler; Marcel Kaiser; Reto Brun
Journal:  Mol Divers       Date:  2009-05-30       Impact factor: 2.943

5.  A chemical biology approach reveals period shortening of the mammalian circadian clock by specific inhibition of GSK-3beta.

Authors:  Tsuyoshi Hirota; Warren G Lewis; Andrew C Liu; Jae Wook Lee; Peter G Schultz; Steve A Kay
Journal:  Proc Natl Acad Sci U S A       Date:  2008-12-22       Impact factor: 11.205

6.  Wnt/β-catenin signaling directs the regional expansion of first and second heart field-derived ventricular cardiomyocytes.

Authors:  Jan Willem Buikema; Ahmed S Mady; Nikhil V Mittal; Ayhan Atmanli; Leslie Caron; Pieter A Doevendans; Joost P G Sluijter; Ibrahim J Domian
Journal:  Development       Date:  2013-09-11       Impact factor: 6.868

7.  β-catenin specifies the endomesoderm and defines the posterior organizer of the hemichordate Saccoglossus kowalevskii.

Authors:  Sébastien Darras; John Gerhart; Mark Terasaki; Marc Kirschner; Christopher J Lowe
Journal:  Development       Date:  2011-03       Impact factor: 6.868

8.  Screening of cell cycle fusion proteins to identify kinase signaling networks.

Authors:  Michelle Trojanowsky; Dusica Vidovic; Scott Simanski; Clara Penas; Stephan Schurer; Nagi G Ayad
Journal:  Cell Cycle       Date:  2015       Impact factor: 4.534

Review 9.  Glycogen synthase kinase 3 (GSK3) in the heart: a point of integration in hypertrophic signalling and a therapeutic target? A critical analysis.

Authors:  P H Sugden; S J Fuller; S C Weiss; A Clerk
Journal:  Br J Pharmacol       Date:  2008-01-21       Impact factor: 8.739

10.  Involvment of cytosolic and mitochondrial GSK-3beta in mitochondrial dysfunction and neuronal cell death of MPTP/MPP-treated neurons.

Authors:  Agnès Petit-Paitel; Frédéric Brau; Julie Cazareth; Joëlle Chabry
Journal:  PLoS One       Date:  2009-05-11       Impact factor: 3.240

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