Abstract
Phosphatases are involved in basically all cellular processes by dephosphorylating cellular components such as proteins, phospholipids and second messengers. They counteract kinases of which many are established oncogenes, and therefore kinases are one of the most important drug targets for targeted cancer therapy. Due to this relationship between kinases and phosphatases, phosphatases are traditionally assumed to be tumour suppressors. However, research findings over the last years prove that this simplification is incorrect, as bona-fide and putative phosphatase oncogenes have been identified. We describe here the role of phosphatases in cancer, tumour suppressors and oncogenes, and their chemical modulators, and discuss new approaches and opportunities for phosphatases as drug targets.
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Abbreviations
- ATM:
-
Ataxia telangiectasia mutated kinase
- BCAR1:
-
Breast cancer antiestrogen resistance 1
- Chk2:
-
Cell cycle checkpoint kinase 2
- DEP-1:
-
Density-enhanced phosphatase-1
- DUSPs:
-
Dual specificity phosphatases
- IZD:
-
Isothiazolidinone
- JMML:
-
Juvenile myelomonocytic leukemia
- LOH:
-
Loss of heterozygosity
- PDZ:
-
PSD95/Dlg/ZO1
- PEST:
-
Domain rich in proline, glutamate, serine and threonine
- PH:
-
Pleckstrin homology
- PHLPP:
-
PH domain leucine-rich repeat protein phosphatases
- PI3K:
-
Phosphatidylinositol-3-kinase
- PIP3:
-
Phosphainositol-3,4,5-trisphosphate
- PKC:
-
Protein kinase C
- PPPs:
-
Phosphoprotein phosphatases
- PRL:
-
Phosphatases of regenerating liver
- PSTKs:
-
Protein serine/threonine kinases
- PSTPs:
-
Protein serine/threonine phosphatases
- PTEN:
-
Phosphatase and tensin homologue deleted on chromosome 10
- PTKs:
-
Protein tyrosine kinases
- PTPs:
-
Protein tyrosine phosphatases
- PTPα or RPTPα:
-
Receptor-like protein tyrosine phosphatase α
- RPTP:
-
Membrane bound receptor like protein tyrosine phosphatase
- SFKs:
-
Src family kinases
- SH2:
-
Src homology 2
- SNPs:
-
Single nucleotide polymorphisms
- TCPTP:
-
T-cell phosphatase
- WIP1:
-
Wild-type p53-induced phosphatase 1
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Fontanillo, M., Köhn, M. (2016). Phosphatases: Their Roles in Cancer and Their Chemical Modulators. In: Böldicke, T. (eds) Protein Targeting Compounds. Advances in Experimental Medicine and Biology, vol 917. Springer, Cham. https://doi.org/10.1007/978-3-319-32805-8_10
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