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Literature DB >> 12031334

Scaffold hopping and optimization towards libraries of glycogen synthase kinase-3 inhibitors.

Lars Naerum¹, Leif Nørskov-Lauritsen, Preben H Olesen.

Abstract

Using a virtual screening strategy based on a methodology derived from the CATS molecular descriptor, a novel compound class with inhibitory activity against the GSK-3 enzyme was identified through scaffold hopping. These compounds were readily synthesized, either by solid-phase or solution-phase chemistry. Compounds with inhibitory activity below 1 microM were identified.

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Year: 2002 PMID： 12031334 DOI： 10.1016/s0960-894x(02)00169-5

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

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Cited

12 in total

1. Protein phosphatase 1 regulates assembly and function of the beta-catenin degradation complex.

Authors: Wen Luo; Annita Peterson; Benjamin A Garcia; Gary Coombs; Bente Kofahl; Reinhart Heinrich; Jeffrey Shabanowitz; Donald F Hunt; H Joseph Yost; David M Virshup
Journal: EMBO J Date: 2007-02-22 Impact factor: 11.598

2. Unregulated mitochondrial GSK3beta activity results in NADH: ubiquinone oxidoreductase deficiency.

Authors: Taj D King; Buffie Clodfelder-Miller; Keri A Barksdale; Gautam N Bijur
Journal: Neurotox Res Date: 2008-12 Impact factor: 3.911

3. Blockade of Tau hyperphosphorylation and Aβ₁₋₄₂ generation by the aminotetrahydrofuran derivative ANAVEX2-73, a mixed muscarinic and σ₁ receptor agonist, in a nontransgenic mouse model of Alzheimer's disease.

Authors: Valentine Lahmy; Johann Meunier; Susanna Malmström; Gaelle Naert; Laurent Givalois; Seung Hyun Kim; Vanessa Villard; Alexandre Vamvakides; Tangui Maurice
Journal: Neuropsychopharmacology Date: 2013-03-14 Impact factor: 7.853

4. The marine natural-derived inhibitors of glycogen synthase kinase-3beta phenylmethylene hydantoins: In vitro and in vivo activities and pharmacophore modeling.

Authors: Mohammad A Khanfar; Bilal Abu Asal; Mudit Mudit; Amal Kaddoumi; Khalid A El Sayed
Journal: Bioorg Med Chem Date: 2009-06-27 Impact factor: 3.641

Scaffold hopping and optimization towards libraries of glycogen synthase kinase-3 inhibitors.

1. Protein phosphatase 1 regulates assembly and function of the beta-catenin degradation complex.

2. Unregulated mitochondrial GSK3beta activity results in NADH: ubiquinone oxidoreductase deficiency.

3. Blockade of Tau hyperphosphorylation and Aβ₁₋₄₂ generation by the aminotetrahydrofuran derivative ANAVEX2-73, a mixed muscarinic and σ₁ receptor agonist, in a nontransgenic mouse model of Alzheimer's disease.

4. The marine natural-derived inhibitors of glycogen synthase kinase-3beta phenylmethylene hydantoins: In vitro and in vivo activities and pharmacophore modeling.

5. Glycogen synthase kinase 3 phosphorylates RBL2/p130 during quiescence.

6. Inhibition of GSK3β-mediated BACE1 expression reduces Alzheimer-associated phenotypes.

7. Adenylate cyclase regulates elongation of mammalian primary cilia.

8. 3D Chemical Similarity Networks for Structure-Based Target Prediction and Scaffold Hopping.

9. Glycogen synthase kinase-3beta (GSK3beta) binds to and promotes the actions of p53.

10. GSK-3 inhibitors induce chromosome instability.