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
Anti-Cancer Agents in Medicinal Chemistry
Title: Dual-Specificity MAP Kinase Phosphatases as Targets of Cancer Treatment
Volume: 11 Issue: 1
Author(s): Caroline Nunes-Xavier, Carlos Roma-Mateo, Pablo Rios, Celine Tarrega, Rocio Cejudo-Marin, Lydia Tabernero and Rafael Pulido
Affiliation:
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
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.
Export Options
About this article
Cite this article as:
Nunes-Xavier Caroline, Roma-Mateo Carlos, Rios Pablo, Tarrega Celine, Cejudo-Marin Rocio, Tabernero Lydia and Pulido Rafael, Dual-Specificity MAP Kinase Phosphatases as Targets of Cancer Treatment, Anti-Cancer Agents in Medicinal Chemistry 2011; 11 (1) . https://dx.doi.org/10.2174/187152011794941190
DOI https://dx.doi.org/10.2174/187152011794941190 |
Print ISSN 1871-5206 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5992 |
Call for Papers in Thematic Issues
Induction of cell death in cancer cells by modulating telomerase activity using small molecule drugs
Telomeres are distinctive but short stretches present at the corners of chromosomes and aid in stabilizing chromosomal makeup. Resynthesis of telomeres supported by the activity of reverse transcriptase ribonucleoprotein complex telomerase. There is no any telomerase activity in human somatic cells, but the stem cells and germ cells undergone telomerase ...read more
Signaling and enzymatic modulators in cancer treatment
Cancer accounts for nearly 10 million deaths in 2022 and is considered the leading cause of worldwide mortality. Cancer outcome can be improved through an appropriate screening and early detection and through an efficient clinical treatment. Chemotherapy, radiotherapy and surgery are the most important approach for the treatment of several ...read more
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
Related Articles
-
Primary Management of Metastatic Colorectal Cancer with Bevacizumab. Review Article Focusing on Efficacy
Current Cancer Therapy Reviews Pharmacology of Cell Adhesion Molecules of the Nervous System
Current Neuropharmacology Targeting the Secretory Pathway for Anti-Inflammatory Drug Development
Current Topics in Medicinal Chemistry Antithrombotic Treatment Management in Patients with Intracerebral Hemorrhage: Reversal and Restart
Current Pharmaceutical Design Hypoxia PET Tracers in EBRT Dose Planning in Head and Neck Cancer
Current Radiopharmaceuticals Vital Elements of the Wnt-Frizzled Signaling Pathway in the Nervous System
Current Neurovascular Research Cerebroprotective Functions of HO-2
Current Pharmaceutical Design Regulation of Angiogenesis by the Small Heat Shock Protein αB-Crystallin
Current Angiogenesis (Discontinued) MicroRNAs in Noise-Induced Hearing Loss and their Regulation by Oxidative Stress and Inflammation
Current Drug Targets COVID-19: Epidemiology, Pathology, Diagnosis, Treatment, and Impact
Current Pharmaceutical Design Placental Cytokines in the Pathogenesis of Preeclampsia and Hellp Syndrome
Current Women`s Health Reviews Coexistence of Ectopic Posterior Pituitary and Sellar/Suprasellar Arachnoid Cyst: A Case Report
Current Medical Imaging Structural Portrait of Filamin Interaction Mechanisms
Current Protein & Peptide Science Assessment and Application of Ultrasound in Ovarian Reserve and Endometrial Receptivity During In vitro Fertilization-embryo Transfer Treatment
Current Medical Imaging The Urokinase Receptor in the Central Nervous System
CNS & Neurological Disorders - Drug Targets Engineered Probiotic and Prebiotic Nutraceutical Supplementations in Combating Non-communicable Disorders: A Review
Current Pharmaceutical Biotechnology Multimodality Imaging in Acute Ischemic Stroke
Current Medical Imaging Recent Strategies Combining Biomaterials and Stem Cells for Bone, Liver and Skin Regeneration
Current Stem Cell Research & Therapy The Network of Fibroblastic Reticular Cells in the Lymph Node:Functional Framework for Immune Surveillance
Current Immunology Reviews (Discontinued) Cardiac Workup of Ischemic Stroke
Current Cardiology Reviews