Abstract
Protein tyrosine phosphatases (PTPs) and their inhibitors have been more and more studied during the past decades. Dephosphorylation is implicated in many biological events including the progression of the cell cycle. Around two hundred PTPs are known in humans, divided into three main groups. They all have a common amino acid sequence in their active site, referred to as the C(X)5R motif, namely a cysteine followed by five varying residues and an arginine. The CDC25 and CDC14 families are examples of PTPs described for their potential in cancer treatment, since they are key regulators of the cell cycle progression. CDC25 inhibitors have already proved their antiproliferative properties whereas the effect of the inhibition of CDC14 remains to be studied.The current review describes how the homology of the active site among the PTPs leads to similarities in their mechanism of action, regulation and inhibition. These similarities make it possible for medicinal chemists to design inhibitors based on the knowledge acquired on PTP1B inhibitors.
Keywords: Protein tyrosine phosphatases, CDC25, CDC14, PTP1B, active site, inhibitor design, enzyme inhibition
Current Enzyme Inhibition
Title: Toward Inhibitors of Protein Tyrosine Phosphatases for Cancer Treatment
Volume: 4 Issue: 1
Author(s): Alban Sidhu, Marie-Odile Contour-Galcera, Dennis Bigg and Gregoire Prevost
Affiliation:
Keywords: Protein tyrosine phosphatases, CDC25, CDC14, PTP1B, active site, inhibitor design, enzyme inhibition
Abstract: Protein tyrosine phosphatases (PTPs) and their inhibitors have been more and more studied during the past decades. Dephosphorylation is implicated in many biological events including the progression of the cell cycle. Around two hundred PTPs are known in humans, divided into three main groups. They all have a common amino acid sequence in their active site, referred to as the C(X)5R motif, namely a cysteine followed by five varying residues and an arginine. The CDC25 and CDC14 families are examples of PTPs described for their potential in cancer treatment, since they are key regulators of the cell cycle progression. CDC25 inhibitors have already proved their antiproliferative properties whereas the effect of the inhibition of CDC14 remains to be studied.The current review describes how the homology of the active site among the PTPs leads to similarities in their mechanism of action, regulation and inhibition. These similarities make it possible for medicinal chemists to design inhibitors based on the knowledge acquired on PTP1B inhibitors.
Export Options
About this article
Cite this article as:
Sidhu Alban, Contour-Galcera Marie-Odile, Bigg Dennis and Prevost Gregoire, Toward Inhibitors of Protein Tyrosine Phosphatases for Cancer Treatment, Current Enzyme Inhibition 2008; 4 (1) . https://dx.doi.org/10.2174/157340808783502559
DOI https://dx.doi.org/10.2174/157340808783502559 |
Print ISSN 1573-4080 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6662 |
- 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
-
Alpha-Particle Microdosimetry
Current Radiopharmaceuticals Recent Progress in the Development of Quinoline Derivatives for the Exploitation of Anti-Cancer Agents
Anti-Cancer Agents in Medicinal Chemistry Role of NF-κB in the Regulation of Cytochrome P450 Enzymes
Current Drug Metabolism Development of Prolactin Receptor Antagonists: Same Goal, Different Ways
Recent Patents on Endocrine, Metabolic & Immune Drug Discovery Nampt/Visfatin/PBEF: A Functionally Multi-faceted Protein with a Pivotal Role in Malignant Tumors
Current Pharmaceutical Design Malignant Mesothelioma Resistance to Apoptosis: Recent Discoveries and their Implication for Effective Therapeutic Strategies
Current Medicinal Chemistry Critical Roles of EGFR Family Members in Breast Cancer and Breast Cancer Stem Cells: Targets for Therapy
Current Pharmaceutical Design Immunotherapy for Prostate Cancer
Current Pharmaceutical Design Role of Netrin-1 Beyond the Brain: From Biomarker of Tissue Injury to Therapy for Inflammatory Diseases
Recent Patents on Biomarkers Anticancer Agents Derived from Natural Products
Mini-Reviews in Medicinal Chemistry Role of Retinoids, Rexinoids and Thyroid Hormone in the Expression of Cytochrome P450 Enzymes
Current Drug Metabolism Breast Cancer: A Review of Risk Factors and New Insights into Treatment
Current Cancer Therapy Reviews Application of NMR Metabolomics to Search for Human Disease Biomarkers
Combinatorial Chemistry & High Throughput Screening The Use of DNA Microarray in the Pharmacogenetics of Antidepressants: Guidelines for a Targeted Approach
Current Genomics The Past, Current Studies and Future of Organometallic <sup>99m</sup>Tc(CO)3 Labeled Peptides and Proteins
Current Pharmaceutical Design A Progressive Review of V600E-B-RAF-Dependent Melanoma and Drugs Inhibiting It
Mini-Reviews in Medicinal Chemistry Glucagon-like Peptides, the Central Nervous System, and the Regulation of Energy Homeostasis
Current Medicinal Chemistry - Central Nervous System Agents Polymer Nanoparticles - A Novel Strategy for Administration of Paclitaxel in Cancer Chemotherapy
Current Medicinal Chemistry Steroid Hybrid Systems: New Molecular Entities with Potential Therapeutical Spectrum
Current Drug Therapy An Overview of the Modulatory Effects of Oleic Acid in Health and Disease
Mini-Reviews in Medicinal Chemistry