Phosphatases: Their Roles in Cancer and Their Chemical Modulators

Part of the Advances in Experimental Medicine and Biology book series (AEMB, volume 917)

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.

Keywords

Phosphatases Cancer Signaling Inhibitors Activators Oncogene Tumor suppressor 

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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Copyright information

© Springer International Publishing Switzerland 2016

Authors and Affiliations

  1. 1.Genome Biology UnitEuropean Molecular Biology LaboratoryHeidelbergGermany

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