p21-Activated kinase 1 (PAK1) has attracted much attention as a potential therapeutic target due to its central role in many oncogenic signaling pathways, its frequent dysregulation in cancers and neurological disorders, and its tractability as a target for small-molecule inhibition. To date, several PAK1-targeting compounds have been developed as preclinical agents, including one that has been evaluated in a clinical trial. A series of ATP-competitive inhibitors, allosteric inhibitors and peptide inhibitors with distinct biochemical and pharmacokinetic properties represent useful laboratory tools for studies on the role of PAK1 in biology and in disease contexts, and could lead to promising therapeutic agents. Given the central role of PAK1 in vital signaling pathways, future clinical development of PAK1 inhibitors will require careful investigation of their safety and efficacy.
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February 2017
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Cover Image
Cover Image
The surface of the catalytic subunit of protein phosphatase PP1 (central 3D-structure) has many binding sites for regulatory proteins that are embedded in regulatory networks (coloured circles linked by lines). Please see pp. 89–99 for more information. Image provided by Mathieu Bollen.
Review Article|
February 15 2017
Targeting PAK1
Galina Semenova;
Galina Semenova
1Cancer Biology Program, Fox Chase Cancer Center, Philadelphia, PA
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Jonathan Chernoff
1Cancer Biology Program, Fox Chase Cancer Center, Philadelphia, PA
Correspondence: Jonathan Chernoff (jonathan.chernoff@fccc.edu)
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Publisher: Portland Press Ltd
Received:
October 03 2016
Revision Received:
November 28 2016
Accepted:
December 01 2016
Online ISSN: 1470-8752
Print ISSN: 0300-5127
© 2017 The Author(s); published by Portland Press Limited on behalf of the Biochemical Society
2017
Biochem Soc Trans (2017) 45 (1): 79–88.
Article history
Received:
October 03 2016
Revision Received:
November 28 2016
Accepted:
December 01 2016
Citation
Galina Semenova, Jonathan Chernoff; Targeting PAK1. Biochem Soc Trans 8 February 2017; 45 (1): 79–88. doi: https://doi.org/10.1042/BST20160134
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