ArticleMethods in molecular biology (Clifton, N.J.)2013
High-throughput screening for protein tyrosine phosphatase activity modulators.
Article in Methods in molecular biology (Clifton, N.J.), 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 papers.
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The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
11 citing papers in PubMed, 10 citations in OpenAlex.
- DUSP family phosphatases in cell signaling, inflammation, and chronic diseases.Journal of biomedical science · 2026Review
- The Binding of 3-O-Methylfluorescein Phosphate to the Catalytic Domain of the Human CDC25B Phosphatase: A Structural Investigation.Chembiochem : a European journal of chemical biology · 2026Article
- Unsaturated Phosphorus Electrophiles to Probe Protein Tyrosine Phosphatases.Angewandte Chemie (International ed. in English) · 2026Article
- False Friends in Fluorescence - Simple HPLC Evaluation of False Positive Fragment Hits in a DiFMUP Assay for Protein Tyrosine Phosphatase 1B.Drug design, development and therapy · 2026Article
- Mitogen-Activated Protein Kinase Phosphatases: No Longer Undruggable?Annual review of pharmacology and toxicology · 2023Review
- Protein Tyrosine Phosphatase Biochemical Inhibition Assays.Bio-protocol · 2022Article
- An allosteric site on MKP5 reveals a strategy for small-molecule inhibition.Science signaling · 2020Article
- A cellular target engagement assay for the characterization of SHP2 (PTPN11) phosphatase inhibitors.The Journal of biological chemistry · 2020Article
- Structural and Functional Characterization of the Histidine Phosphatase Domains of Human Sts-1 and Sts-2.Biochemistry · 2017Article
- Functional Analysis of Protein Tyrosine Phosphatases in Thrombosis and Hemostasis.Methods in molecular biology (Clifton, N.J.) · 2016Article
- Perspective: Tyrosine phosphatases as novel targets for antiplatelet therapy.Bioorganic & medicinal chemistry · 2015Review
Corrections and comments
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Authors and funding
2 authors at 1 institution in 1 country.
Funding
Abstract
Reversible phosphorylation of proteins, principally on serine, threonine, or tyrosine residues, is central to the regulation of most aspects of eukaryotic cell function. Dysregulation of protein kinases and protein phosphatases is linked to numerous human diseases. Consequently, many efforts have been made to target these enzymes with small molecules in order to develop new therapeutic agents. While protein kinase inhibitors have been successfully brought to the market, the development of specific protein phosphatase inhibitors is still in its infancy. The largest and most diverse protein phosphatase superfamily in humans is comprised by the protein tyrosine phosphatases, a group of over 100 enzymes. Here, we describe high-throughput screening methods to search for protein tyrosine phosphatase activity modulators. We illustrate the implementation of relatively simple phosphatase assays, using generic absorbance- or fluorescence-based substrates, in 384- or 1536-well microtiter plates. We discuss steps to optimize HTS assay quality and performance, and describe several PTP screening methods on the basis of previously performed successful HTS campaigns. Finally, we discuss how to confirm, follow up, and prioritize hit compounds, and point out a number of common pitfalls that are encountered in this process.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.