Protein tyrosine phosphatases: New markers and targets in oncology?

Abstract

It is now clear that PTPS have both inhibitory and stimulatory effects on cancer-associated signalling processes, and depending on their associated proteins and substrates, they act as oncogenes in multiple human cancers. Soon, several ongoing studies should validate PTPS such as PTEN and PTPN1 as useful prognostic markers and potentially novel targets in cancer therapies. Although much current interest surrounds the clinical introduction of specific PTK inhibitors, chemical targeting of PTPS remains largely unexplored. Despite major efforts by the pharmaceutical industry (given that these targets were identified more than 10 years after the tyrosine kinases), the development of small-molecule inhibitors of PTPS is still in its early stages. Phosphatases represent 4% of the "drug-able" human genome, and the rapidly increasing number of human diseases associated with PTP abnormalities - including cancer - has begun to elicit a growing interest in PTPS as drug targets in oncology. The recent identification of PTPN1 as a potential oncogene in breast cancer may be key in focusing research efforts toward this relatively poorly known gene family. Copyright © 2008 Multimed Inc.