Please use this identifier to cite or link to this item: https://www.um.edu.mt/library/oar/handle/123456789/24128
Title: Deregulation of the protein phosphatase 2A, PP2A in cancer : complexity and therapeutic options
Authors: Grech, Godfrey
Baldacchino, Shawn
Saliba, Christian
Grixti, Maria Pia
Gauci, Robert
Petroni, Vanessa
Fenech, Anthony G.
Scerri, Christian
Keywords: Phosphoprotein phosphatases
Breast -- Cancer
Colon (Anatomy) -- Cancer
Nitric oxide
Issue Date: 2016
Publisher: Springer
Citation: Grech, G., Baldacchino, S., Saliba, C., Grixti, M. P., Gauci, R., Petroni, V., ...Scerri, C. (2016). Deregulation of the protein phosphatase 2A, PP2A in cancer: complexity and therapeutic options. Tumor Biology, 37(9), 11691-11700.
Abstract: The complexity of the phosphatase, PP2A, is being unravelled and current research is increasingly providing information on the association of deregulated PP2A function with cancer initiation and progression. It has been reported that decreased activity of PP2A is a recurrent observation in many types of cancer, including colorectal and breast cancer (Baldacchino et al. EPMA J. 5:3, 2014; Cristobal et al. Mol Cancer Ther. 13:938–947, 2014). Since deregulation of PP2A and its regulatory subunits is a common event in cancer, PP2A is a potential target for therapy (Baldacchino et al. EPMA J. 5:3, 2014). In this review, the structural components of the PP2A complex are described, giving an in depth overview of the diversity of regulatory subunits. Regulation of the active PP2A trimeric complex, through phosphorylation and methylation, can be targeted using known compounds, to reactivate the complex. The endogenous inhibitors of the PP2A complex are highly deregulated in cancer, representing cases that are eligible to PP2A-activating drugs. Pharmacological opportunities to target low PP2A activity are available and preclinical data support the efficacy of these drugs, but clinical trials are lacking.We highlight the importance of PP2A deregulation in cancer and the current trends in targeting the phosphatase.
URI: https://www.um.edu.mt/library/oar//handle/123456789/24128
Appears in Collections:Scholarly Works - CenMMB
Scholarly Works - FacM&SCPT
Scholarly Works - FacM&SPat
Scholarly Works - FacM&SPB

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