2013年12月7日土曜日

Protein Phosphatase-Directed Therapeutics　２０１６


Approaches to Study Phosphatases

† European Molecular Biology Laboratory, Genome Biology Unit, Meyerhofstrasse 1, 69117 Heidelberg, Germany
ACS Chem. Biol., 2016, 11 (11), pp 2944–2961
DOI: 10.1021/acschembio.6b00570
Publication Date (Web): October 4, 2016
Copyright © 2016 American Chemical Society
*E-mail: koehn@embl.de.
 ACS AuthorChoice - This is an open access article published under an ACS AuthorChoice License, which permits copying and redistribution of the article or any adaptations for non-commercial purposes.

Abstract

Abstract Image
 
 
 
Phosphatases play key roles in normal physiology and diseases. Studying phosphatases has been both essential and challenging, and the application of conventional genetic and biochemical methods has led to crucial but still limited understanding of their mechanisms, substrates, and exclusive functions within highly intricate networks. With the advances in technologies such as cellular imaging and molecular and chemical biology in terms of sensitive tools and methods, the phosphatase field has thrived in the past years and has set new insights for cell signaling studies and for therapeutic development. In this review, we give an overview of the existing interdisciplinary tools for phosphatases, give examples on how they have been applied to increase our understanding of these enzymes, and suggest how they—and other tools yet barely used in the phosphatase field—might be adapted to address future questions and challenges.

Supporting Information

The Supporting Information is available free of charge on the ACS Publications website at DOI: 10.1021/acschembio.6b00570.
  • Abbreviations, Glossary, and Supporting Table 1 (PDF)

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Article Views: 1,341 Times
Received 1 July 2016
Date accepted 12 September 2016
Published online 4 October 2016
Published in print 18 November 2016
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Abstract Image


Protein phosphatases have both protective and promoting roles in the etiology of diseases. A prominent example is the existence of oncogenic as well as tumor-suppressing protein phosphatases.

 

A few protein phosphatase activity modulators are already applied in therapies. These were however not developed in target-directed approaches, and the recent discovery of phosphatase involvement followed their application in therapy.

 

Nevertheless, these examples demonstrate that small molecules can be generated that modulate the activity of protein phosphatases and are beneficial for the treatment of protein phosphorylation diseases.

 

 

We describe here strategies for the development of activators and inhibitors of protein phosphatases and clarify some long-standing misconceptions concerning the druggability of these enzymes.

 

Recent developments suggest that it is feasible to design potent and selective protein phosphatase modulators with a therapeutic potential.

 
 
 
http://pubs.acs.org/doi/abs/10.1021/cb300597g?prevSearch=%2528ERK%2Binhibitor%2529%2Band%2B%255BAbstract%253A%2Bsmall%255D&searchHistoryKey=
 
 
 
 
 
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