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Recent discovery and development of protein tyrosine phosphatase inhibitors

2002; Taylor & Francis; Volume: 12; Issue: 6 Linguagem: Inglês

10.1517/13543776.12.6.871

1744-7674

Hwa-Ok Kim, Mark A. T. Blaskovich,

RNA modifications and cancer

AbstractThe protein tyrosine phosphatases (PTPases or PTPs) play an important role in controlling the status of tyrosine phosphorylation and the regulation of cellular function. The ability to selectively inhibit PTPs holds enormous therapeutic potential for the treatment of diseases such as diabetes, cancer and osteoporosis. However, an understanding of the role of many PTPs has yet to be unravelled, with only PTP1B convincingly validated as a therapeutic target. Furthermore, the intricate network of different PTPs extensively involved in signalling events requires high selectivity for the desired PTP target, in order to minimise potential side effects. Most research programmes into PTP inhibitors are still at an early stage and have yet to convert initial leads into compounds with more drug-like properties. Inhibitors have been identified by modification of peptide substrates, from natural product screening and by rational design. This article will give an overview of PTPs, followed by a more detailed description of the development of PTP inhibitors. Patents on PTP inhibitors published between January 1998 and Feb 2002 will be discussed in the context of the available literature.KeywordscancerCD45cdc25hyperglycaemiainsulin resistanceLARobesityprotein tyrosine phosphataseprotein tyrosine phosphatase inhibitorPTP1BTCPTPType II diabetesVHR