Covalent Inhibitors of Protein Tyrosine Phosphatases (original) (raw)

Abstract

The importance of a carefully regulated protein dephosphorylation event in cellular signaling by protein tyrosine phosphatases (PTPs) is well recognized. Indeed an anomalous level of PTP activities has been associated with a variety of aberrant cellular signaling and human diseases. As a result of this, potent and selective inhibitory agents of PTP enzymes are sought after by research communities across the globe. While there is considerable interest among academic researchers and pharmaceutical industries to develop non-covalent and reversible inhibitory agents of PTPs, the development of covalent inhibitory agents is plagued with presumption that they are not suitable candidates for drug discovery. This outcome is primarily due to the concern that such molecules could be immunogenic and serve as cellular toxic agents. The current success of covalent therapeutic agents in clinics, however, does not support this notion, and indicates that there is a need to reconsider this hypothesi...

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