Current Pharmacology Reports

, Volume 4, Issue 3, pp 238–249 | Cite as

Inhibitors of the p21 Activated Kinases

  • Namrata Sampat
  • Audrey Minden
Kinase Inhibitor (A Minden, Section Editor)
Part of the following topical collections:
  1. Topical Collection on Kinase Inhibitor


This review article provides an overview of some of the inhibitors that have been generated against the p21-activated kinases (PAKs). Immunohistopathological evaluation, gene profiling studies, and functional assays have indicated that PAKs play important roles in human diseases, particularly cancer. Many tumor samples that have been evaluated have shown overexpression or amplification of PAK genes. Furthermore, several studies have also shown that PAKs are involved in brain diseases as well as infectious diseases. Since the PAK kinases have been linked to cancer and other diseases, they are often considered to be valuable therapeutic targets. A number of PAK inhibitors are currently under study for their use in research or as therapeutic agents. In some cases, promising results have been obtained from both in vivo and in vitro studies. Studies are ongoing to assess the specificity of PAK inhibitors toward specific PAK isoforms, to determine their pharmacokinetic profiles, and to determine optimal doses. Future studies will determine which PAK inhibitors will be the most promising candidates for clinical development.


PAKs p21 activated kinase PAK inhibitors Kinase inhibitors Cancer 


Compliance with Ethical Standards

Conflict of Interest Statement

On behalf of all authors, the corresponding author indicates that there is no conflict of interest.

Human and Animal Rights and Informed Consent

This article does not contain any studies with human or animal subjects performed by any of the authors.


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Copyright information

© Springer International Publishing AG, part of Springer Nature 2018

Authors and Affiliations

  1. 1.Susan Lehman Cullman Laboratory for Cancer Research, Department of Chemical Biology, Ernest Mario School of Pharmacy, RutgersThe State University of New JerseyPiscatawayUSA

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