FCCC LOGO Faculty Publications
Targeting PAK1
Biochem Soc Trans. 2017 Feb 08;45(1) :79-88
PMID: 28202661    PMCID: PMC5973817    URL: https://www.ncbi.nlm.nih.gov/pubmed/28202661
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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.
1470-8752 Semenova, Galina Chernoff, Jonathan Journal Article Review England Biochem Soc Trans. 2017 Feb 8;45(1):79-88. doi: 10.1042/BST20160134.