Glycogen Synthase Kinase-3 (GSK-3)-Targeted Therapy and Imaging
作者： Mukesh K. Pandey , Timothy R. DeGrado
DOI: 10.7150/THNO.14334
关键词:
摘要: Glycogen synthase kinase-3 (GSK-3) is associated with various key biological processes, including glucose regulation, apoptosis, protein synthesis, cell signaling, cellular transport, gene transcription, proliferation, and intracellular communication. Accordingly, GSK-3 has been implicated in a wide variety of diseases specifically targeted for both therapeutic imaging applications by large number academic laboratories pharmaceutical companies. Here, we review the structure, function, expression levels, ligand-binding properties its connection to diseases. A selected list highly potent inhibitors, IC50 <20 nM adenosine triphosphate (ATP)-competitive inhibitors <5 μM non-ATP-competitive were analyzed structure activity relationships. Furthermore, ubiquitous possible impact on therapy are also highlighted. Finally, rational perspective route selective effective discussed.
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Diana Alonso, Ana Martnez, Marine Compounds as a New Source for Glycogen Synthase Kinase 3 Inhibitors John Wiley & Sons, Inc.. pp. 307- 331 ,(2006) , 10.1002/0470052171.CH16
Eléonore Beurel, Marjelo A Mines, Ling Song, Richard S Jope, Glycogen synthase kinase-3 levels and phosphorylation undergo large fluctuations in mouse brain during development Bipolar Disorders. ,vol. 14, pp. 822- 830 ,(2012) , 10.1111/BDI.12023
Noor EMBI, Dennis B. RYLATT, Philip COHEN, Glycogen Synthase Kinase-3 from Rabbit Skeletal Muscle FEBS Journal. ,vol. 107, pp. 519- 527 ,(2005) , 10.1111/J.1432-1033.1980.TB06059.X
Günter U Höglinger, Hans‐Jürgen Huppertz, Stefan Wagenpfeil, María V Andrés, Vincente Belloch, Teresa León, Teodoro Del Ser, TAUROS MRI Investigators, JC Gmez, B Tijero, R Villoria, J García de Yebenes, JL Lopez Sendón, E Tolosa, MT Buongiorno, N Bargalló, JA Burguera, I Martinez, J Ruiz‐Martínez, J Villanua, F Vivancos, I Ybot, M Aguilar, JL Dolz, M Boada, A Lafuente, MA Tejero, JJ López‐Lozano, M Mata, A Kupsch, A Lipp, M Höllerhage, WH Oertel, G Respondek, M Stamelou, S Knake, D Berg, W Maetzler, KK Srulijes, A Gröger, A Ludolph, J Kassubek, M Steiger, K Tyler, DJ Burn, L Morris, A Lees, H Ling, L Strycharczuk, None, Tideglusib reduces progression of brain atrophy in progressive supranuclear palsy in a randomized trial. Movement Disorders. ,vol. 29, pp. 479- 487 ,(2014) , 10.1002/MDS.25815
Philip Cohen, James R. Woodgett, Multisite phosphorylation of glycogen synthase Biochimica et Biophysica Acta (BBA) - Protein Structure and Molecular Enzymology. ,vol. 788, pp. 339- 347 ,(1984) , 10.1016/0167-4838(84)90047-5
Teodoro del Ser, Klaus C. Steinwachs, Hermann J. Gertz, María V. Andrés, Belén Gómez-Carrillo, Miguel Medina, Joan A. Vericat, Pilar Redondo, David Fleet, Teresa León, Treatment of Alzheimer's disease with the GSK-3 inhibitor tideglusib: a pilot study. Journal of Alzheimer's Disease. ,vol. 33, pp. 205- 215 ,(2012) , 10.3233/JAD-2012-120805
Eduardo Tolosa, Irene Litvan, Günter U Höglinger, David Burn, Andrew Lees, María V Andrés, Belén Gómez‐Carrillo, Teresa León, Teodoro Del Ser, TAUROS Investigators, JC Gómez, B Tijero, K Berganzo, J García de Yebenes, JL Lopez Sendón, G Garcia, E Tolosa, MT Buongiorno, N Bargalló, JA Burguera, I Martinez, J Ruiz‐Martínez, I Narrativel, F Vivancos, I Ybot, M Aguilar, P Quilez, M Boada, A Lafuente, I Hernandez, JJ López‐Lozano, M Mata, A Kupsch, A Lipp, G Ebersbach, T Schmidt, K Hahn, G Höglinger, M Höllerhage, WH Oertel, G Respondek, M Stamelou, H Reichmann, M Wolz, C Schneider, L Klingelhöfer, D Berg, W Maetzler, KK Srulijes, A Ludolph, J Kassubek, M Steiger, K Tyler, DJ Burn, L Morris, A Lees, H Ling, R Hauser, T McClain, D Truong, S Jenkins, I Litvan, D Houghton, J Ferrara, Y Bordelon, A Gratiano, L Golbe, M Mark, R Uitti, J Ven Gerpen, None, A phase 2 trial of the GSK-3 inhibitor tideglusib in progressive supranuclear palsy Movement Disorders. ,vol. 29, pp. 470- 478 ,(2014) , 10.1002/MDS.25824
Tarek MK Motawi, Yasser Bustanji, Shohda A EL‐Maraghy, Mutasem O Taha, Mohamed AS Al Ghussein, None, Naproxen and cromolyn as new glycogen synthase kinase 3β inhibitors for amelioration of diabetes and obesity: an investigation by docking simulation and subsequent in vitro/in vivo biochemical evaluation. Journal of Biochemical and Molecular Toxicology. ,vol. 27, pp. 425- 436 ,(2013) , 10.1002/JBT.21503
Claudie Hooper, Richard Killick, Simon Lovestone, The GSK3 hypothesis of Alzheimer's disease. Journal of Neurochemistry. ,vol. 104, pp. 1433- 1439 ,(2008) , 10.1111/J.1471-4159.2007.05194.X
James A. McCubrey, Linda S. Steelman, Fred E. Bertrand, Nicole M. Davis, Melissa Sokolosky, Steve L. Abrams, Giuseppe Montalto, Antonino B. D’Assoro, Massimo Libra, Ferdinando Nicoletti, Roberta Maestro, Jorg Basecke, Dariusz Rakus, Agnieszka Gizak, Zoya Demidenko, Lucio Cocco, Alberto M. Martelli, Melchiorre Cervello, GSK-3 as potential target for therapeutic intervention in cancer. Oncotarget. ,vol. 5, pp. 2881- 2911 ,(2014) , 10.18632/ONCOTARGET.2037