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Abstract
<jats:p>Protein tyrosyl phosphorylation is a dynamic reversible regulatory process that is es-sential for virtually all aspects of cellular function. Dysregulation of protein tyrosyl phosphorylation is one of the main causes of human diseases such as cancer, diabetes, autoimmune disorders, and neurological diseases. Protein tyrosine kinases (PTKs) have paved the way towards defining the significance of protein tyrosyl phosphorylation in human health and disease. However, homeostatic control of protein tyrosyl phosphor-ylation is also regulated by protein tyrosine phosphatases (PTPs). The actions of PTPs are diverse functioning to both positively and negatively regulate signaling pathways through specific substrate dephosphorylation. The PTKs are now matured targets with numerous drugs that have been developed for the treatment of human diseases such as cancer and immunological disorders. In contrast, PTPs are relatively in their infancy as compared with their PTK counterparts with regards to drug development for the treatment of human diseases. However, mounting evidence supports the view that PTPs are not only valid targets but are indeed targetable. This review will highlight recent developments in the PTP field which provide support for the emergence of PTPs as therapeutic targets for diseases such as cancer, obesity, type II diabetes and rare diseases.</jats:p>