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
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 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.