Abstract
p21-Activated kinases (PAKs) are positioned at the nexus of several oncogenic signalling pathways. Overexpression or mutational activation of PAK isoforms frequently occurs in various human tumours, and recent data suggest that excessive PAK activity drives many of the cellular processes that are the hallmarks of cancer. In this Review, we discuss the mechanisms of PAK activation in cancer, the key substrates that mediate the developmental and oncogenic effects of this family of kinases, and how small-molecule inhibitors of these enzymes might be best developed and deployed for the treatment of cancer.
Publication types
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Research Support, N.I.H., Extramural
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Research Support, U.S. Gov't, Non-P.H.S.
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Review
MeSH terms
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Animals
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Antineoplastic Agents / pharmacology
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Disease Progression
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Enzyme Activation
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Gene Amplification
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Humans
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Neoplasm Invasiveness
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Neoplasm Metastasis
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Neoplasms / drug therapy
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Neoplasms / enzymology*
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Neoplasms / genetics
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Neoplasms / pathology
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Neovascularization, Pathologic / enzymology
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Protein Kinase Inhibitors / pharmacology
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p21-Activated Kinases / antagonists & inhibitors
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p21-Activated Kinases / genetics
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p21-Activated Kinases / metabolism*
Substances
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Antineoplastic Agents
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Protein Kinase Inhibitors
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p21-Activated Kinases