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- Title
Targeting PAK1.
- Authors
Semenova, Galina; Chernoff, Jonathan
- Abstract
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 smallmolecule 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.
- Subjects
PROTEIN kinases; ONCOGENIC proteins; CANCER treatment; NEUROLOGICAL disorders; SMALL molecules; CLINICAL trials
- Publication
Biochemical Society Transactions, 2017, Vol 45, Issue 1, p79
- ISSN
0300-5127
- Publication type
Article
- DOI
10.1042/BST20160134