Literature DB >> 17355201

A high throughput luminescent assay for glycogen synthase kinase-3beta inhibitors.

Andrea Baki1, Attila Bielik, László Molnár, Györgyi Szendrei, György M Keserü.   

Abstract

A high throughput luminescent assay based on the Kinase-Glo() system (Promega, Madison, WI) has been developed for screening against glycogen synthase kinase-3beta (GSK-3beta). Careful optimization of assay parameters allowed us to develop a robust, reproducible, and sensitive assay. Its usefulness has been demonstrated in a high throughput screening run when screening 55,000 compounds. This campaign yielded five chemical classes of hits, including several highly potent GSK-3beta inhibitors.

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Year:  2007        PMID: 17355201     DOI: 10.1089/adt.2006.029

Source DB:  PubMed          Journal:  Assay Drug Dev Technol        ISSN: 1540-658X            Impact factor:   1.738


  26 in total

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2.  Citrus flavonoids luteolin, apigenin, and quercetin inhibit glycogen synthase kinase-3β enzymatic activity by lowering the interaction energy within the binding cavity.

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Journal:  J Med Food       Date:  2011-04       Impact factor: 2.786

3.  Consensus models for CDK5 inhibitors in silico and their application to inhibitor discovery.

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Journal:  Mol Divers       Date:  2014-12-16       Impact factor: 2.943

4.  1,5-Benzothiazepine Derivatives: Green Synthesis, In Silico and In Vitro Evaluation as Anticancer Agents.

Authors:  Michelyne Haroun; Santosh S Chobe; Rajasekhar Reddy Alavala; Savita M Mathure; Risy Namratha Jamullamudi; Charushila K Nerkar; Vijay Kumar Gugulothu; Christophe Tratrat; Mohammed Monirul Islam; Katharigatta N Venugopala; Mohammed Habeebuddin; Mallikarjun Telsang; Nagaraja Sreeharsha; Md Khalid Anwer
Journal:  Molecules       Date:  2022-06-10       Impact factor: 4.927

5.  Crosstalk between phosphodiesterase 7 and glycogen synthase kinase-3: two relevant therapeutic targets for neurological disorders.

Authors:  Jose A Morales-Garcia; Valle Palomo; Miriam Redondo; Sandra Alonso-Gil; Carmen Gil; Ana Martinez; Ana Perez-Castillo
Journal:  ACS Chem Neurosci       Date:  2014-01-17       Impact factor: 4.418

6.  Dual GSK-3β/AChE Inhibitors as a New Strategy for Multitargeting Anti-Alzheimer's Disease Drug Discovery.

Authors:  Xue-Yang Jiang; Ting-Kai Chen; Jun-Ting Zhou; Si-Yu He; Hong-Yu Yang; Yao Chen; Wei Qu; Feng Feng; Hao-Peng Sun
Journal:  ACS Med Chem Lett       Date:  2018-02-09       Impact factor: 4.345

7.  Glycogen synthase kinase-3 inhibitors as potent therapeutic agents for the treatment of Parkinson disease.

Authors:  J A Morales-García; C Susín; S Alonso-Gil; D I Pérez; V Palomo; C Pérez; S Conde; A Santos; C Gil; A Martínez; A Pérez-Castillo
Journal:  ACS Chem Neurosci       Date:  2012-12-05       Impact factor: 4.418

8.  Fangchinoline suppresses the growth and invasion of human glioblastoma cells by inhibiting the kinase activity of Akt and Akt-mediated signaling cascades.

Authors:  Bingyu Guo; Peng Xie; Jingyuan Su; Tingting Zhang; Xiaoming Li; Guobiao Liang
Journal:  Tumour Biol       Date:  2015-09-25

9.  Isolation, structure elucidation and total synthesis of lajollamide A from the marine fungus Asteromyces cruciatus.

Authors:  Tobias A M Gulder; Hanna Hong; Jhonny Correa; Ekaterina Egereva; Jutta Wiese; Johannes F Imhoff; Harald Gross
Journal:  Mar Drugs       Date:  2012-12       Impact factor: 5.118

10.  Protein kinase CK-1 inhibitors as new potential drugs for amyotrophic lateral sclerosis.

Authors:  Irene G Salado; Miriam Redondo; Murilo L Bello; Concepción Perez; Nicole F Liachko; Brian C Kraemer; Laetitia Miguel; Magalie Lecourtois; Carmen Gil; Ana Martinez; Daniel I Perez
Journal:  J Med Chem       Date:  2014-03-12       Impact factor: 7.446

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