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Proteinaceous Regulators and Inhibitors of Protein Tyrosine Phosphatases
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Molecules 2018, 23(3), 569; https://doi.org/10.3390/molecules23030569

Targeting Receptor-Type Protein Tyrosine Phosphatases with Biotherapeutics: Is Outside-in Better than Inside-Out?

1
Institute of Cardiovascular Sciences, College of Medical and Dental Sciences, University of Birmingham, Birmingham B15 2TT, UK
2
Department of Biomedical Science, Faculty of Science and Technology, University of Westminster, London W1W 6UW, UK
*
Author to whom correspondence should be addressed.
Received: 30 January 2018 / Revised: 26 February 2018 / Accepted: 26 February 2018 / Published: 2 March 2018
(This article belongs to the Special Issue Protein-Tyrosine Phosphatase Inhibitors)
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Abstract

Protein tyrosine phosphatases (PTPs), of the receptor and non-receptor classes, are key signaling molecules that play critical roles in cellular regulation underlying diverse physiological events. Aberrant signaling as a result of genetic mutation or altered expression levels has been associated with several diseases and treatment via pharmacological intervention at the level of PTPs has been widely explored; however, the challenges associated with development of small molecule phosphatase inhibitors targeting the intracellular phosphatase domain (the “inside-out” approach) have been well documented and as yet there are no clinically approved drugs targeting these enzymes. The alternative approach of targeting receptor PTPs with biotherapeutic agents (such as monoclonal antibodies or engineered fusion proteins; the “outside-in” approach) that interact with the extracellular ectodomain offers many advantages, and there have been a number of exciting recent developments in this field. Here we provide a brief overview of the receptor PTP family and an update on the emerging area of receptor PTP-targeted biotherapeutics for CD148, vascular endothelial-protein tyrosine phosphatase (VE-PTP), receptor-type PTPs σ, γ, ζ (RPTPσ, RPTPγ, RPTPζ) and CD45, and discussion of future potential in this area. View Full-Text
Keywords: tyrosine phosphatase; receptor; phosphorylation; ectodomain; biotherapeutic; biological; inhibitor; disease tyrosine phosphatase; receptor; phosphorylation; ectodomain; biotherapeutic; biological; inhibitor; disease
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).
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Senis, Y.A.; Barr, A.J. Targeting Receptor-Type Protein Tyrosine Phosphatases with Biotherapeutics: Is Outside-in Better than Inside-Out? Molecules 2018, 23, 569.

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