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Inhibitors of glycogen synthase kinase-3: future therapy for unmet medical needs?

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Pages 1527-1536 | Published online: 25 Feb 2005

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Read on this site (3)

Fereshteh Shiri, Alireza Shahraki & Massoud Nejati-Yazdinejad. (2020) 3D-QSAR and Molecular Docking Study on Maleimide-Based Glycogen Synthase Kinase 3 (GSK-3) Inhibitors as Stimulators of Steroidogenesis. Polycyclic Aromatic Compounds 40:3, pages 743-757.
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Valle Palomo & Ana Martinez. (2017) Glycogen synthase kinase 3 (GSK-3) inhibitors: a patent update (2014-2015). Expert Opinion on Therapeutic Patents 27:6, pages 657-666.
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Yasser Bustanji, Mutasem O. Taha, Ihab M. Almasri, Mohamed A.S. Al-Ghussein, Mohammad K. Mohammad & Hatim S. Alkhatib. (2009) Inhibition of glycogen synthase kinase by curcumin: Investigation by simulated molecular docking and subsequent in vitro/in vivo evaluation. Journal of Enzyme Inhibition and Medicinal Chemistry 24:3, pages 771-778.
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Articles from other publishers (41)

Shan-Kui Liu, Hong-Xu Xie, Yong-Xi Ge, Juan Zhang & Cheng-Shi Jiang. (2021) An updated research of glycogen synthase kinase-3β inhibitors: a review. Monatshefte für Chemie - Chemical Monthly 152:1, pages 19-33.
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Daniel Drießen, Fabian Stuhldreier, Annika Frank, Holger Stark, Sebastian Wesselborg, Björn Stork & Thomas J.J. Müller. (2019) Novel meriolin derivatives as rapid apoptosis inducers. Bioorganic & Medicinal Chemistry 27:15, pages 3463-3468.
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M. Xu, S.L. Wang, L. Zhu, P.Y. Wu, W.B. Dai & K.P. Rakesh. (2019) Structure-activity relationship (SAR) studies of synthetic glycogen synthase kinase-3β inhibitors: A critical review. European Journal of Medicinal Chemistry 164, pages 448-470.
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Sandeep R. Kunati, Shuming Yang, David Wald & Yan Xu. (2018) Development and validation of an LC–MS/MS method for quantitative determination of GS87, a novel antineoplastic agent, in mouse plasma. Journal of Pharmaceutical and Biomedical Analysis 153, pages 145-151.
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A. Prasanth Saraswati, S.M. Ali Hussaini, Namballa Hari Krishna, Bathini Nagendra Babu & Ahmed Kamal. (2018) Glycogen synthase kinase-3 and its inhibitors: Potential target for various therapeutic conditions. European Journal of Medicinal Chemistry 144, pages 843-858.
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Przemysław Czeleń. (2017) Inhibition mechanism of CDK-2 and GSK-3β by a sulfamoylphenyl derivative of indoline—a molecular dynamics study. Journal of Molecular Modeling 23:8.
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Przemysław Czeleń. (2016) Molecular dynamics study on inhibition mechanism of CDK-2 and GSK-3β by CHEMBL272026 molecule. Structural Chemistry 27:6, pages 1807-1818.
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Przemysław Czeleń & Beata Szefler. (2015) Molecular dynamics study of the inhibitory effects of ChEMBL474807 on the enzymes GSK-3β and CDK-2. Journal of Molecular Modeling 21:4.
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Sergiy A Starosyla. (2014) Pharmacophore approaches in protein kinase inhibitors design. World Journal of Pharmacology 3:4, pages 162.
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Prinka Singla, Vijay Luxami & Kamaldeep Paul. (2014) Benzimidazole-biologically attractive scaffold for protein kinase inhibitors. RSC Advances 4:24, pages 12422.
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Ritesh Agrawal, Pratima Jain, Subodh Narayan Dikshit, Radhe Shyam Bahare & Swastika Ganguly. (2013) Ligand-based pharmacophore detection, screening of potential pharmacophore and docking studies, to get effective glycogen synthase kinase inhibitors. Medicinal Chemistry Research 22:11, pages 5504-5535.
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Anna N. Parker, Matthew J. Lock & John M. Hutchison. (2013) Synthesis of 4-benzyl-3-phenylbutenolide natural products. Tetrahedron Letters 54:39, pages 5322-5324.
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Sukanta Kamila & Edward R. Biehl. (2012) Microwave-assisted synthesis of novel bis(2-thioxothiazolidin-4-one) derivatives as potential GSK-3 inhibitors. Tetrahedron Letters 53:31, pages 3998-4003.
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Nihar R. Jena. (2011) Binding of BIS like and other ligands with the GSK-3β kinase: a combined docking and MM-PBSA study. Journal of Molecular Modeling 18:2, pages 631-644.
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Shao-Yong Lu, Yong-Jun Jiang, Jing Lv, Jian-Wei Zou & Tian-Xing Wu. (2011) Role of bridging water molecules in GSK3β-inhibitor complexes: Insights from QM/MM, MD, and molecular docking studies. Journal of Computational Chemistry 32:9, pages 1907-1918.
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Sergey Arutyunyan & Adel Nefzi. (2010) Synthesis of Chiral Polyaminothiazoles. Journal of Combinatorial Chemistry 12:3, pages 315-317.
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Marie Laronze-Cochard, Fabien Cochard, Etienne Daras, Amélie Lansiaux, Bertrand Brassart, Enguerran Vanquelef, Elise Prost, Jean-Marc Nuzillard, Brigitte Baldeyrou, Jean-François Goosens, Olivier Lozach, Laurent Meijer, Jean-François Riou, Eric Henon & Janos Sapi. (2010) Synthesis and biological evaluation of new penta- and heptacyclic indolo- and quinolinocarbazole ring systems obtained via Pd0 catalysed reductive N-heteroannulation. Organic & Biomolecular Chemistry 8:20, pages 4625.
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Ana Martinez. (2008) Preclinical efficacy on GSK‐3 inhibitors: Towards a future generation of powerful drugs. Medicinal Research Reviews 28:5, pages 773-796.
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Viney Lather, Rajendra Kristam, Jagmohan Singh Saini, Rajendra Kristam, Narasingapuram Arumugam Karthikeyan & Vitukudi Narayana Balaji. (2008) QSAR Models for Prediction of Glycogen Synthase Kinase‐3β Inhibitory Activity of Indirubin Derivatives. QSAR & Combinatorial Science 27:6, pages 718-728.
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Mutasem O. Taha, Yasser Bustanji, Mohamed A. S. Al-Ghussein, Mohammad Mohammad, Hiba Zalloum, Ihab M. Al-Masri & Naji Atallah. (2008) Pharmacophore Modeling, Quantitative Structure–Activity Relationship Analysis, and in Silico Screening Reveal Potent Glycogen Synthase Kinase-3β Inhibitory Activities for Cimetidine, Hydroxychloroquine, and Gemifloxacin. Journal of Medicinal Chemistry 51:7, pages 2062-2077.
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Yasushi Miyazaki, Yutaka Maeda, Hideyuki Sato, Masato Nakano & Geoffrey W. Mellor. (2008) Rational design of 4-amino-5,6-diaryl-furo[2,3-d]pyrimidines as potent glycogen synthase kinase-3 inhibitors. Bioorganic & Medicinal Chemistry Letters 18:6, pages 1967-1971.
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Mark Hamann, Diana Alonso, Ester Martín-Aparicio, Ana Fuertes, M. José Pérez-Puerto, Ana Castro, Susana Morales, María Luisa Navarro, María del Monte-Millán, Miguel Medina, Hari Pennaka, Akula Balaiah, Jiangnan Peng, Jennifer Cook, Subagus Wahyuono & Ana Martínez. (2007) Glycogen Synthase Kinase-3 (GSK-3) Inhibitory Activity and Structure–Activity Relationship (SAR) Studies of the Manzamine Alkaloids. Potential for Alzheimer’s Disease. Journal of Natural Products 70:9, pages 1397-1405.
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Han-Cheng Zhang, Llorente V.R. Boñaga, Hong Ye, Claudia K. Derian, Bruce P. Damiano & Bruce E. Maryanoff. (2007) Novel bis(indolyl)maleimide pyridinophanes that are potent, selective inhibitors of glycogen synthase kinase-3. Bioorganic & Medicinal Chemistry Letters 17:10, pages 2863-2868.
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Kumaran G. Sreejalekshmi, Satyabhama K.C. Devi & Kallikat N. Rajasekharan. (2006) An efficient protocol for solid phase aminothiazole synthesis. Tetrahedron Letters 47:35, pages 6179-6182.
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Carlos A. ZarateJrJr, Jaskaran Singh & Husseini K. Manji. (2006) Cellular Plasticity Cascades: Targets for the Development of Novel Therapeutics for Bipolar Disorder. Biological Psychiatry 59:11, pages 1006-1020.
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Ana MartinezMercedes AlonsoAna CastroIsabel DorronsoroJ. Luis GelpíF. Javier LuqueConcepción PérezFrancisco J. Moreno. (2005) SAR and 3D-QSAR Studies on Thiadiazolidinone Derivatives:  Exploration of Structural Requirements for Glycogen Synthase Kinase 3 Inhibitors. Journal of Medicinal Chemistry 48:23, pages 7103-7112.
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Rosario Luna-Medina, Marta Cortes-Canteli, Mercedes Alonso, Angel Santos, Ana Martínez & Ana Perez-Castillo. (2005) Regulation of Inflammatory Response in Neural Cells in Vitro by Thiadiazolidinones Derivatives through Peroxisome Proliferator-activated Receptor γ Activation. Journal of Biological Chemistry 280:22, pages 21453-21462.
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Cédrik Garino, Frédéric Bihel, Nicolas Pietrancosta, Younes Laras, Gilles Quéléver, Irene Woo, Peter Klein, Jenny Bain, Jean-Luc Boucher & Jean-Louis Kraus. (2005) New 2-bromomethyl-8-substituted-benzo[c]chromen-6-ones. Synthesis and biological properties. Bioorganic & Medicinal Chemistry Letters 15:1, pages 135-138.
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V.M. Dembitsky, H. Abu Ali & M. Srebnik. 2005. Contemporary Aspects of Boron: Chemistry and Biological Applications. Contemporary Aspects of Boron: Chemistry and Biological Applications 119 297 .
L. Meijer, M. Leost, O. Lozach, S. Schmitt & C. Kunick. 2005. Inhibitors of Protein Kinases and Protein Phosphates. Inhibitors of Protein Kinases and Protein Phosphates 47 64 .
T D Gould, J A Quiroz, J Singh, C A ZarateJrJr & H K Manji. (2004) Emerging experimental therapeutics for bipolar disorder: insights from the molecular and cellular actions of current mood stabilizers. Molecular Psychiatry 9:8, pages 734-755.
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Han-Cheng Zhang, Hong Ye, Bruce R. Conway, Claudia K. Derian, Michael F. Addo, Gee-Hong Kuo, Leonard R. Hecker, Diane R. Croll, Jian Li, Lori Westover, Jun Z. Xu, Richard Look, Keith T. Demarest, Patricia Andrade-Gordon, Bruce P. Damiano & Bruce E. Maryanoff. (2004) 3-(7-Azaindolyl)-4-arylmaleimides as potent, selective inhibitors of glycogen synthase kinase-3. Bioorganic & Medicinal Chemistry Letters 14:12, pages 3245-3250.
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David J. O'Neill, Lan Shen, Catherine Prouty, Bruce R. Conway, Lori Westover, Jun Z. Xu, Han-Cheng Zhang, Bruce E. Maryanoff, William V. Murray, Keith T. Demarest & Gee-Hong Kuo. (2004) Design, synthesis, and biological evaluation of novel 7-azaindolyl-heteroaryl-maleimides as potent and selective glycogen synthase kinase-3β (GSK-3β) inhibitors. Bioorganic & Medicinal Chemistry 12:12, pages 3167-3185.
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Lan Shen, Catherine Prouty, Bruce R. Conway, Lori Westover, Jun Z. Xu, Richard A. Look, Xin Chen, Mary Pat Beavers, Jerry Roberts, William V. Murray, Keith T. Demarest & Gee-Hong Kuo. (2004) Synthesis and biological evaluation of novel macrocyclic bis-7-azaindolylmaleimides as potent and highly selective glycogen synthase kinase-3β (GSK-3β) inhibitors. Bioorganic & Medicinal Chemistry 12:5, pages 1239-1255.
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Panagiotis PolychronopoulosProkopios MagiatisAlexios-Leandros SkaltsounisVassilios MyrianthopoulosEmmanuel MikrosAldo TarriconeAndrea MusacchioS. Mark RoeLaurence PearlMaryse LeostPaul GreengardLaurent Meijer. (2004) Structural Basis for the Synthesis of Indirubins as Potent and Selective Inhibitors of Glycogen Synthase Kinase-3 and Cyclin-Dependent Kinases. Journal of Medicinal Chemistry 47:4, pages 935-946.
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Todd D Gould, Guang Chen & Husseini K Manji. (2003) In Vivo Evidence in the Brain for Lithium Inhibition of Glycogen Synthase Kinase-3. Neuropsychopharmacology 29:1, pages 32-38.
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Laurent Meijer, Alexios-Leandros Skaltsounis, Prokopios Magiatis, Panagiotis Polychronopoulos, Marie Knockaert, Maryse Leost, Xiaozhou P. Ryan, Claudia Alin Vonica, Ali Brivanlou, Rana Dajani, Claudia Crovace, Cataldo Tarricone, Andrea Musacchio, S.Mark Roe, Laurence Pearl & Paul Greengard. (2003) GSK-3-Selective Inhibitors Derived from Tyrian Purple Indirubins. Chemistry & Biology 10:12, pages 1255-1266.
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Santiago Conde, Daniel I. Pérez, Ana Martínez, Concepción Perez & Francisco J. Moreno. (2003) Thienyl and Phenyl α-Halomethyl Ketones:  New Inhibitors of Glycogen Synthase Kinase (GSK-3β) from a Library of Compound Searching. Journal of Medicinal Chemistry 46:22, pages 4631-4633.
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Gee-Hong Kuo, Catherine Prouty, Alan DeAngelis, Lan Shen, David J. O'Neill, Chandra Shah, Peter J. Connolly, William V. Murray, Bruce R. Conway, Peter Cheung, Lori Westover, Jun Z. Xu, Richard A. Look, Keith T. Demarest, Stuart Emanuel, Steven A. Middleton, Linda Jolliffe, Mary Pat Beavers & Xin Chen. (2003) Synthesis and Discovery of Macrocyclic Polyoxygenated Bis-7-azaindolylmaleimides as a Novel Series of Potent and Highly Selective Glycogen Synthase Kinase-3β Inhibitors. Journal of Medicinal Chemistry 46:19, pages 4021-4031.
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Jason Witherington, Vincent Bordas, Alessandra Gaiba, Antoinette Naylor, Anthony D. Rawlings, Brian P. Slingsby, David G. Smith, Andrew K. Takle & Robert W. Ward. (2003) 6-Heteroaryl-pyrazolo[3,4-b]pyridines: potent and selective inhibitors of glycogen synthase kinase-3 (GSK-3). Bioorganic & Medicinal Chemistry Letters 13:18, pages 3059-3062.
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Han-Cheng Zhang, Kimberly B. White, Hong Ye, David F. McComsey, Claudia K. Derian, Michael F. Addo, Patricia Andrade-Gordon, Annette J. Eckardt, Bruce R. Conway, Lori Westover, Jun Z. Xu, Richard Look, Keith T. Demarest, Stuart Emanuel & Bruce E. Maryanoff. (2003) Macrocyclic bisindolylmaleimides as inhibitors of protein kinase C and glycogen synthase kinase-3. Bioorganic & Medicinal Chemistry Letters 13:18, pages 3049-3053.
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