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

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.

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