Abstract
Reversible protein tyrosine phosphorylation, catalysed by the counter-actors protein tyrosine phosphatases (PTPs) and protein tyrosine kinases (PTKs), is a fundamentally important regulatory mechanism of proteins in living cells, controlling cell communication, proliferation, differentiation, motility, and molecular trafficking. The activities of PTPs and PTKs are derailed in several diseases such as cancer and type II diabetes, making them attractive drug targets. Developing drugs against PTKs has started a decade earlier than that on PTPs, and at present there are several molecules targeting PTKs on the market. PTPs in turn are of raising interest, with PTP1B on the lead for its effects on type II diabetes and obesity. In the search for modulators of PTP activity, high-throughput methods are important as the initial step to find suitable lead compounds for drug development. Also, high-throughput methods are very useful in elucidating the specific function of different PTPs. In this review, the different high-throughput studies performed to find inhibitors and activators of classical PTPs are discussed.
Keywords: High throughput screens (HTS), TCPTP, SHP-2, LAR, LYP, CD45, RTK, DiFMUP, pNPP, HTS, OMFP
Anti-Cancer Agents in Medicinal Chemistry
Title: High-Throughput Methods in Identification of Protein Tyrosine Phosphatase Inhibitors and Activators
Volume: 11 Issue: 1
Author(s): Elina Mattila and Johanna Ivaska
Affiliation:
Keywords: High throughput screens (HTS), TCPTP, SHP-2, LAR, LYP, CD45, RTK, DiFMUP, pNPP, HTS, OMFP
Abstract: Reversible protein tyrosine phosphorylation, catalysed by the counter-actors protein tyrosine phosphatases (PTPs) and protein tyrosine kinases (PTKs), is a fundamentally important regulatory mechanism of proteins in living cells, controlling cell communication, proliferation, differentiation, motility, and molecular trafficking. The activities of PTPs and PTKs are derailed in several diseases such as cancer and type II diabetes, making them attractive drug targets. Developing drugs against PTKs has started a decade earlier than that on PTPs, and at present there are several molecules targeting PTKs on the market. PTPs in turn are of raising interest, with PTP1B on the lead for its effects on type II diabetes and obesity. In the search for modulators of PTP activity, high-throughput methods are important as the initial step to find suitable lead compounds for drug development. Also, high-throughput methods are very useful in elucidating the specific function of different PTPs. In this review, the different high-throughput studies performed to find inhibitors and activators of classical PTPs are discussed.
Export Options
About this article
Cite this article as:
Mattila Elina and Ivaska Johanna, High-Throughput Methods in Identification of Protein Tyrosine Phosphatase Inhibitors and Activators, Anti-Cancer Agents in Medicinal Chemistry 2011; 11 (1) . https://dx.doi.org/10.2174/187152011794941235
DOI https://dx.doi.org/10.2174/187152011794941235 |
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
-
The Power of Enzyme Kinetics in the Drug Development Process
Current Pharmaceutical Biotechnology Process Variables and Design of Experiments in Liposome and Nanoliposome Research
Mini-Reviews in Medicinal Chemistry How Much Gets there and What Does it Do?: The Need for Better Pharmacokinetic and Pharmacodynamic Endpoints in Contemporary Drug Discovery and Development
Current Pharmaceutical Design Inflammation and Anemia
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry Cardiovascular and Systemic Risk in Nonalcoholic Fatty Liver Disease - Atherosclerosis as a Major Player in the Natural Course of NAFLD
Current Pharmaceutical Design Personalized and Predictive Medicine in Turkey: A Symposium Report of the Istanbul Working Group on Personalized Medicine, Istanbul, Turkey, September 10-12, 2009
Current Pharmacogenomics and Personalized Medicine High Dose Immunoglobulin (IVIG) May Reduce the Incidence of Langerhans Cell Histiocytosis (LCH)-Associated Central Nervous System Involvement
CNS & Neurological Disorders - Drug Targets Targeting CCK Receptors in Human Cancers
Current Topics in Medicinal Chemistry Green Synthesis of Silver Nanoparticle using Sechium edule Aqueous Extract and Study of Antimicrobial and Catalytic Activity
Current Nanomaterials Synthesis of Cross-linked Poly (N-isopropylacrylamide) Magnetic Nano Composite for Application in the Controlled Release of Doxorubicin
Pharmaceutical Nanotechnology Network Effect of Wt-mutant p53 Interactions and Implications on p53 Gene Therapy
Current Pharmaceutical Design Synthesis and Structure-activity Relationships of Chalcone Derivatives as Inhibitors of Ovarian Cancer Cell Growth
Letters in Drug Design & Discovery Recent Developments in Breast Tomosynthesis Imaging
Recent Patents on Medical Imaging Recent Developments in Anti-Cancer Agents Targeting the Ras/Raf/ MEK/ERK Pathway
Recent Patents on Anti-Cancer Drug Discovery The Peripheral Benzodiazepine Receptor: A Promising Therapeutic Drug Target
Current Medicinal Chemistry Prospects for Gene Therapy of Osteopetrosis
Current Gene Therapy Drug Repurposing in Chemical Genomics: Can We Learn from the Past to Improve the Future?
Current Topics in Medicinal Chemistry Morphological and Functional Characteristic of Senescent Cancer Cells
Current Drug Targets Virus-Associated Vasculitides: An Update
Current Immunology Reviews (Discontinued) Pluripotency Crossroads: Junction of Transcription Factors, Epigenetic Mechanisms, MicroRNAs, and Long Non-coding RNAs
Current Stem Cell Research & Therapy