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p21-activated kinase family: promising new drug targets

Authors Huynh N, He H

Received 25 February 2015

Accepted for publication 1 April 2015

Published 14 May 2015 Volume 2015:5 Pages 119—128

DOI https://doi.org/10.2147/RRBC.S57278

Checked for plagiarism Yes

Review by Single-blind

Peer reviewer comments 4

Editor who approved publication: Professor Nikolay Dokholyan

Nhi Huynh, Hong He

Department of Surgery, University of Melbourne, Austin Health, Melbourne, VIC, Australia

Abstract: The p21-activated kinase (PAK) family of serine/threonine protein kinases are downstream effectors of the Rho family of GTPases. PAKs are frequently upregulated in human diseases, including various cancers, and their overexpression correlates with disease progression. Current research findings have validated important roles for PAKs in cell proliferation, survival, gene transcription, transformation, and cytoskeletal remodeling. PAKs are shown to act as a converging node for many signaling pathways that regulate these cellular processes. Therefore, PAKs have emerged as attractive targets for treatment of disease. This review discusses the physiological and pathological roles of PAKs, validation of PAKs as new promising drug targets, and current challenges and advances in the development of PAK-targeted anticancer therapy, with a focus on PAKs and human cancers.

Keywords: p21-activated kinase, cancer, inhibitor

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