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 |
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
Role of natural compounds as anti anti-cancer agents
Cancer is considered the leading cause of worldwide mortality, accounting for nearly 10 million deaths in 2022. Cancer outcome can be improved through an appropriate screening and early detection and through an efficient clinical treatment. Chemotherapy remains an important approach in treatment o f several types of cancers, even though ...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
-
Tea (Camellia sinensis (L.)): A Putative Anticancer Agent in Bladder Carcinoma?
Anti-Cancer Agents in Medicinal Chemistry Novel Monocyte Biomarkers of Atherogenic Conditions
Current Pharmaceutical Design The Pim Kinases: New Targets for Drug Development
Current Drug Targets Natural Products in Structure-Assisted Design of Molecular Cancer Therapeutics
Current Pharmaceutical Design Focused Microarray Analysis: Characterization of Phenomes by Gene Expression Profiling
Current Pharmacogenomics Viral Vectors for Gene-Directed Enzyme Prodrug Therapy
Current Gene Therapy In vivo Cancer Imaging with Semiconductor Quantum Dots
Current Pharmaceutical Analysis The Secretin/Pituitary Adenylate Cyclase-Activating Polypeptide/ Vasoactive Intestinal Polypeptide Superfamily in the Central Nervous System
Central Nervous System Agents in Medicinal Chemistry Cancer Drug Development with the Help of Radiopharmaceuticals: Academic Experience
Current Pharmaceutical Design Pharmacological Approaches to Targeting Muscarinic Acetylcholine Receptors
Recent Patents on CNS Drug Discovery (Discontinued) Induction of Abscopal Anti-Tumor Immunity and Immunogenic Tumor Cell Death by Ionizing Irradiation - Implications for Cancer Therapies
Current Medicinal Chemistry Cannabinoid Hyperemesis Syndrome
Current Drug Abuse Reviews A Review on Noscapine, and its Impact on Heme Metabolism
Current Drug Metabolism Pharmacogenomics of Cytochrome P450 Enzymes in Tumours
Current Pharmacogenomics Calreticulin is Differentially Expressed in Invasive Ductal Carcinoma: A Comparative Study
Current Proteomics Growth Retardation in Children with Celiac Disease
Current Pediatric Reviews Patent Selections:
Recent Patents on Anti-Cancer Drug Discovery Gold Nanoparticles - Synthesis and Applications in Cancer Management
Recent Patents on Materials Science Interleukin-15 in Gene Therapy of Cancer
Current Gene Therapy Synthetic Lipoproteins as Carriers for Drug Delivery
Current Medicinal Chemistry