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Target intelligence / Profile preview
p21-Activated Kinase Group II Isoforms (PAK Group II)
- Target
- PAK Group II
- Molecular classification
- Serine/threonine protein kinase, Enzyme
01
Overview
p21-activated kinases (PAKs) are a family of serine/threonine protein kinases that act as key effectors for the Rho GTPases Cdc42 and Rac. Group II PAKs include PAK4, PAK5 (also known as PAK7), and PAK6. They regulate several fundamental cellular processes including cytoskeletal organization, cell cycle progression, cell survival/apoptosis regulation, cell adhesion and motility. They play particularly important roles in development, neuronal function, and cancer biology, especially in gastrointestinal cancers, making them attractive drug targets. Their activity is controlled by a pseudosubstrate motif at their N terminus.
- Other names
- PAK4/5/6Group II PAKsPAK Group IIPAK4PAK5PAK6
02
Mechanism of action
Inhibition of kinase activity
03
Biological functions
Cytoskeletal organizationCell cycle progressionCell survival/apoptosis regulationCell adhesionCell motilityDevelopmentNeuronal function
04
Disease associations
CancerGastrointestinal cancers
05
Safety considerations
Lack of high selectivity of inhibitorsSuboptimal drug-like properties of inhibitors
06
Interacting drugs
GNE 2861
1 more in the full profile.
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