Protein tyrosine phosphatases (PTPs) counteract the enzymatic activity of protein tyrosine kinases to modulate levels of both normal and disease-associated protein tyrosine phosphorylation. Aberrant activity of PTPs has been linked to the progression of many disease states, yet no PTP inhibitors are currently clinically available. PTPs are without a doubt a difficult drug target. Despite this, many selective, potent, and bioavailable PTP inhibitors have been described, suggesting PTPs should once again be looked at as viable therapeutic targets. Herein, we summarize recently discovered PTP inhibitors and their use in the functional interrogation of PTPs in disease states. In addition, an overview of the therapeutic targeting of PTPs is described using SHP2 as a representative target.
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Review Article| August 25 2021
Functional interrogation and therapeutic targeting of protein tyrosine phosphatases
Aaron D. Krabill;
Department of Medicinal Chemistry and Molecular Pharmacology, Department of Chemistry, and Institute for Drug Discovery, Purdue University, West Lafayette, IN 47907, U.S.A.
Correspondence: Zhong-Yin Zhang (firstname.lastname@example.org)
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Aaron D. Krabill, Zhong-Yin Zhang; Functional interrogation and therapeutic targeting of protein tyrosine phosphatases. Biochem Soc Trans 27 August 2021; 49 (4): 1723–1734. doi: https://doi.org/10.1042/BST20201308
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