High-Throughput Methods in Identification of Protein Tyrosine Phosphatase Inhibitors and Activators

ISSN: 1875-5992 (Online)
ISSN: 1871-5206 (Print)

Volume 17, 14 Issues, 2017

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Anti-Cancer Agents in Medicinal Chemistry

Formerly: Current Medicinal Chemistry - Anti-Cancer Agents

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Michelle Prudhomme
Institut de Chimie de Clermont-Ferrand
Université Clermont Auvergne

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High-Throughput Methods in Identification of Protein Tyrosine Phosphatase Inhibitors and Activators

Anti-Cancer Agents in Medicinal Chemistry, 11(1): 141-150.

Author(s): Elina Mattila and Johanna Ivaska.

Affiliation: VTT Medical Biotechnology, Itainen Pitkakatu 4C, Turku FIN-20520, Finland.


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.


High throughput screens (HTS), TCPTP, SHP-2, LAR, LYP, CD45, RTK, DiFMUP, pNPP, HTS, OMFP.

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Article Details

Volume: 11
Issue Number: 1
First Page: 141
Last Page: 150
Page Count: 10
DOI: 10.2174/187152011794941235

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