Dual-Specificity MAP Kinase Phosphatases as Targets of Cancer Treatment

ISSN: 1875-5992 (Online)
ISSN: 1871-5206 (Print)


Volume 16, 12 Issues, 2016


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Anti-Cancer Agents in Medicinal Chemistry

Formerly: Current Medicinal Chemistry - Anti-Cancer Agents

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Editor-in-Chief:
Michelle Prudhomme
Universite Blaise Pascal - C.N.R.S
Aubiere Cedex
France


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Dual-Specificity MAP Kinase Phosphatases as Targets of Cancer Treatment



Anti-Cancer Agents in Medicinal Chemistry, 11(1): 109-132.

Author(s): Caroline Nunes-Xavier, Carlos Roma-Mateo, Pablo Rios, Celine Tarrega, Rocio Cejudo-Marin, Lydia Tabernero and Rafael Pulido.

Affiliation: Centro de Investigacion Principe Felipe, Avda. Autopista del Saler 16-3, 46013 Valencia, Spain.

Abstract

The protein tyrosine phosphatase family (PTP) contains a group of dual-specificity phosphatases (DUSPs) that regulate the activivity of MAP kinases (MAPKs), which are key effectors in the control of cell growth and survival in physiological and pathological processes, including cancer. These phosphatases, named as MKP-DUSPs, include the MAPK phosphatases (MKPs) as well as a group of small-size atypical DUSPs structurally and functionally related to the MKPs. MKP-DUSPs, in most of the cases, are direct inactivators of MAPKs by dephosphorylation of both the Thr and the Tyr regulatory residues at the MAPKs catalytic loop. In some other cases, MKPDUSPs regulate the activity of MAPKs indirectly, acting through upstream MAPK pathways components. The active involvement of MKP-DUSPs in oncogenesis or resistance to cancer therapies is now well documented, making the search and validation of MKP-DUSPs inhibitors a prominent area in clinical cancer research. Here, we review the current knowledge on the role of MKP-DUSPs in human cancer, the status of the preclinical development and validation of specific MKP-DUSP inhibitors, and the potential of MKP-DUSPs as targets for anti-cancer drugs.

Keywords:

Protein tyrosine phosphatases (PTPs), dual-specificity phosphatases (DUSPs), MAP kinase phosphatases (MKPs), inhibitors, anti-cancer agents, JNK1, VRK3, ERK1/2, dual specificity, LNCaP, PMA.



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Article Details

Volume: 11
Issue Number: 1
First Page: 109
Last Page: 132
Page Count: 24
DOI: 10.2174/187152011794941190
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