Abstract
Protein tyrosine phosphatases (PTPs) are key regulatory enzymes in signal transduction pathways and their aberrancy has been implicated in various diseases such as cancers, metabolic syndromes, and autoimmune disorders. In spite of its great importance, determination of the functional significance of PTPs remains a major challenge, and efficient methodologies are needed to specifically delineate PTP functions. Besides the strategy to use potent and selective PTP inhibitors to study the physiological roles of the enzymes, measurement of PTP activities using specific PTP substrates or activity-based probes (ABPs) has been reported. This review focused on the recent development of small molecular probes to detect PTP activities, consisting of five sub-categories: 1. Conventional fluorescent substrates; 2. Ratiometric fluorescent PTP substrates; 3. Fluorescence substrates with selectivity to a single PTP or a class of PTPs; 4. ABPs specific for PTPs; and 5. A real-time imaging of PTP-substrate complex using a small molecule PTP probe which, offers a measurement of a real-time activity of a certain PTP in cells.
Keywords: DiFMUP, in-gel assay, phosphotyrosine, dual-specificity PTP (DUSP), Forster resonance energy transfer (FRET), 4-fluoromethylphenylphosphate (FMPP), 2-fluoromethylphosphotyrosine (FMPT), PTKs, PTPs, Pnpp
Anti-Cancer Agents in Medicinal Chemistry
Title: Recent Advances in Protein Tyrosine Phosphatase Detection Using Chemical Probes
Volume: 11 Issue: 1
Author(s): Kyeong Lee, Hyo Jin Kang, Yan Xia and Sang J. Chung
Affiliation:
Keywords: DiFMUP, in-gel assay, phosphotyrosine, dual-specificity PTP (DUSP), Forster resonance energy transfer (FRET), 4-fluoromethylphenylphosphate (FMPP), 2-fluoromethylphosphotyrosine (FMPT), PTKs, PTPs, Pnpp
Abstract: Protein tyrosine phosphatases (PTPs) are key regulatory enzymes in signal transduction pathways and their aberrancy has been implicated in various diseases such as cancers, metabolic syndromes, and autoimmune disorders. In spite of its great importance, determination of the functional significance of PTPs remains a major challenge, and efficient methodologies are needed to specifically delineate PTP functions. Besides the strategy to use potent and selective PTP inhibitors to study the physiological roles of the enzymes, measurement of PTP activities using specific PTP substrates or activity-based probes (ABPs) has been reported. This review focused on the recent development of small molecular probes to detect PTP activities, consisting of five sub-categories: 1. Conventional fluorescent substrates; 2. Ratiometric fluorescent PTP substrates; 3. Fluorescence substrates with selectivity to a single PTP or a class of PTPs; 4. ABPs specific for PTPs; and 5. A real-time imaging of PTP-substrate complex using a small molecule PTP probe which, offers a measurement of a real-time activity of a certain PTP in cells.
Export Options
About this article
Cite this article as:
Lee Kyeong, Jin Kang Hyo, Xia Yan and J. Chung Sang, Recent Advances in Protein Tyrosine Phosphatase Detection Using Chemical Probes, Anti-Cancer Agents in Medicinal Chemistry 2011; 11 (1) . https://dx.doi.org/10.2174/187152011794941208
DOI https://dx.doi.org/10.2174/187152011794941208 |
Print ISSN 1871-5206 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5992 |
- 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
-
Gonadotropin-Releasing Hormone Receptor Signaling: Biased and Unbiased
Mini-Reviews in Medicinal Chemistry Lipid Based Nanosystems for Curcumin: Past, Present and Future
Current Pharmaceutical Design Platycodin D Induces Tumor Growth Arrest by Activating FOXO3a Expression in Prostate Cancer in vitro and in vivo
Current Cancer Drug Targets Downstream Carcinogenesis Signaling Pathways by Green Tea Polyphenols: A Translational Perspective of Chemoprevention and Treatment for Cancers
Current Drug Metabolism Nanomedicine based on Nucleic Acids: Pharmacokinetic and Pharmacodynamic Perspectives
Current Pharmaceutical Biotechnology Nanoparticles for Cancer Targeting: Current and Future Directions
Current Drug Delivery Hypothyroidism and Cardiovascular Disease: Factors, Mechanism and Future Perspectives
Current Medicinal Chemistry Integrated, Molecular Engineering Approaches to Develop Prostate Cancer Gene Therapy
Current Gene Therapy Involvement of IL-1R/TLR Signalling in Experimental Autoimmune Encephalomyelitis and Multiple Sclerosis
Current Molecular Medicine Notch Signaling in Cardiovascular Disease and Calcification
Current Cardiology Reviews Alzheimer’s Disease And Type 2 Diabetes: Exploring The Association To Obesity And Tyrosine Hydroxylase
CNS & Neurological Disorders - Drug Targets C-11 Radiochemistry in Cancer Imaging Applications
Current Topics in Medicinal Chemistry Selenium and Cardiovascular Surgery: An Overview
Current Drug Safety Anti-Inflammatory and Pro-Resolving Effects of N-3 PUFA in Cancers: Structures and Mechanisms
Current Topics in Medicinal Chemistry Tualang Honey and its Methanolic Fraction Improve LPS-induced Learning and Memory Impairment in Male Rats: Comparison with Memantine
Current Nutrition & Food Science Small-Molecule CSF1R Inhibitors as Anticancer Agents
Current Medicinal Chemistry UPA and PAI-1 Analysis from Fixed Tissues – New Perspectives for a Known Set of Predictive Markers
Current Medicinal Chemistry C-20 Cyclopropyl Vitamin D3 Analogs
Current Topics in Medicinal Chemistry Metal Containing Cytostatics and Their Interaction with Cellular Thiol Compounds Causing Chemoresistance
Anti-Cancer Agents in Medicinal Chemistry The Role of Melatonin in the Immuno-Neuro-Psychology of Mental Disorders
Recent Patents on CNS Drug Discovery (Discontinued)