KEY GSK-3 PUBLICATIONS
To learn more about the role of GSK-3β in cancer, please see these resources.
Review
Molecular Pathways: Revisiting Glycogen Synthase Kinase-3β as a Target for the Treatment of Cancer
Clinical Cancer Research, 2017; DOI: 10.1158/1078-0432.CCR-15-2240; Amy Walz, Andrey Ugolkov, Sunandana Chandra, Alan Kozikowski, Benedito A. Carneiro, Thomas V. ,O’Halloran, Francis J. Giles, Daniel D. Billadeau, and Andrew P. Mazar
Targeting GSK-3: a promising approach for cancer therapy?
Future Oncology, 2006; 2(1):91-100; Ougolkov A, Billadeau DD.
Glioblastoma
Combination treatment with the GSK-3 inhibitor 9-ING-41 and CCNU cures orthotopic chemoresistant glioblastoma in patient-derived xenograft models
Translational Oncology; 2017 Aug; 10(4):669-678; Andrey Ugolkov, Wenan Qiang, Gennadiy Bondarenko, Daniel Procissi, Irina Gaisina, C. David James, James Chandler, Alan Kozikowski, HendraGunosewoyo, Thomas O’Halloran, Jeffry Raizer and Andrew P. Mazar
Potential therapeutic effect of glycogen synthase kinase 3β inhibition against human glioblastoma.
Clin Cancer Res 2009; 15:887-897; Miyashita K, Kawakami K, Nakada M, Mai W, Shakoori A, Fujisawa H, Hayashi Y, Hamada J, Minamoto T.
GSK3β regulates differentiation and growth arrest in glioblastoma
PLoS One 2009;4(10):e7443; Korur S, Huber RM, Sivasankaran B, Petrich M, Morin P Jr, Hemmings BA, Merlo A, Lino MM.
Glycogen synthase kinase-3 inhibition induces glioma cell death through c-MYC, nuclear factor-κB, and glucose regulation.
Cancer Res 2008; 68(16):6643-6651; Kotliarova S, Pastorino S, Kovell LC, Kotliarov Y, Song H, Zhang W, Bailey R, Maric D, Zenklusen JC, Lee J, Fine HA.
Pancreatic Cancer
Glycogen synthase kinase-3β ablation limits pancreatitis-induced acinar-to-ductal metaplasia
Journal of Pathology; 2017 Sep; 243(1):65-77; Li Ding, Geou-Yarh Liou, Daniel M Schmitt, Peter Storz, Jin-San Zhang and Daniel D Billadeau
Glycogen synthase kinase-3β participates in nuclear factor kappaB-mediated gene transcription and cell survival in pancreatic cancer cells.
Cancer Res, 2005; 65:2076-2081; Ougolkov A, Fernandez-Zapico M, Savoy D, Urrutia R, Billadeau D.
From a natural product lead to the identification of potent and selective benzofuran-3-yl-(indol-3-yl)maleimides as glycogen synthase kinase 3β inhibitors that suppress proliferation and survival of pancreatic cancer cells.
J Med Chem 2009; 52:1853-1863; Gaisina I, Gallier F, Ougolkov A, Kim K, Kurome T, Guo S, Holzle D, Luchini D, Blond S, Billadeau D, Kozikowski A.
Aberrant nuclear accumulation of glycogen synthase kinase-3β in human pancreatic cancer: association with kinase activity and tumor dedifferentiation.
Clin Cancer Res 2006; 12:5074-5081; Ougolkov A, Fernandez-Zapico M, Bilim V, Smyrk T, Chari S, Billadeau D.
Breast cancer
GSK-3 inhibition overcomes chemoresistance in human breast cancer
Cancer Letters, 2016; 380:384–392; Andrey Ugolkov, Irina Gaisina, Jin-San Zhang, Daniel D. Billadeau, Kevin White, Alan Kozikowski, Sarika Jain, Massimo Cristofanilli, Francis Giles, Thomas O’Halloran, Vincent L. Cryns, Andrew P. Mazar
Glycogen synthase kinase-3β positively regulates protein synthesis and cell proliferation through the regulation of translation initiation factor 4E-binding protein 1.
Oncogene 2014; 33:1690-99; Shin S, Wolgamott L, Tcherkezian J, Vallabhapurapu S, Yu Y, Roux PP, et al.
Ovarian cancer
Glycogen synthase kinase 3β inhibitors induce apoptosis in ovarian cancer cells and inhibit in-vivo tumor growth.
Anticancer Drugs 2011; 22:978-985; Hilliard T, Gaisina I, Muehlbauer A, Gaisin A, Gallier F, Burdette J.
Leukemia
Inhibition of glycogen synthase kinase-3 activity leads to epigenetic silencing of nuclear factor κB target genes and induction of apoptosis in chronic lymphocytic leukemia B cells.
Blood 2007; 110:735-74; Ougolkov A, Bone N, Fernandez-Zapico M, Kay N, Billadeau D.
Glycogen synthase kinase 3 in MLL leukaemia maintenance and targeted therapy.
Nature 2008; 455(7217):1205-1209; Wang Z, Smith KS, Murphy M, Piloto O, Somervaille T, Cleary M.
Renal Cancer
Glycogen synthase kinase-3: a new therapeutic target in renal cell carcinoma.
Br J Cancer 2009; 101:2005-2014; Bilim V, Ougolkov A, Yuuki K, Naito S, Kawazoe H, Muto A, Oya M, Billadeau D, Motoyama T, Tomita Y.
Inhibition of GSK-3 induces differentiation and impaired glucose metabolism in renal cancer.
Mol Cancer Ther 2014; 13(2):285-296; Pal K, Ying C, Gaisina IN., Bhattacharya S, Dutta SK, Wang E, Gunosewoyo H, Kozikowski AP, Billadeau DD, Mukhopadhyay D.
Bladder Cancer
Glycogen synthase kinase-3β: a prognostic marker and a potential therapeutic target in human bladder cancer.
Clin Cancer Res 2010; 16(21):5124-5132; Naito S, Bilim V, Yuuki K, Ugolkov A, Motoyama T, Nagaoka A, Kato T, Tomita Y.
Colon Cancer
Deregulated GSK3β activity in colorectal cancer: its association with tumor cell survival and proliferation.
Biochem Biophys Res Commun 2005; 334:1365-1373; Ougolkov A, Shakoori A, Zhang B, Modarressi M, Billadeau D, Mai M, Takahashi Y, Minamoto T.
Thyroid Cancer
Inactivation of glycogen synthase kinase-3β, a downstream target of the raf-1 pathway, is associated with growth suppression in medullary thyroid cancer cells.
Mol Cancer Ther 2007; 6:1151-1158; Kunnimalaiyaan M, Vaccaro A, Ndiaye M, Chen H.
Prostate cancer
Suppression of glycogen synthase kinase 3 activity reduces tumor growth of prostate cancer in vivo.
Prostate 2011; 71:835-845; Zhu Q, Yang J, Han S, Liu J, Holzbeierlein J, Thrashe, J, Li B.