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Target intelligence / Profile preview
Serine/threonine-protein kinase PAK 2 (PAK2)
- Target
- PAK2
- Molecular classification
- Enzyme, Kinase, Serine/threonine kinase, Signal transduction protein
01
Overview
Serine/threonine-protein kinase PAK 2 (PAK2) is a member of the p21-activated kinase family that acts as an effector for small Rho GTPases, including CDC42 and RAC1, playing key roles in the regulation of the cytoskeleton, cell motility, adhesion, cell cycle progression, apoptotic signaling, and cell survival[2][4][8]. PAK2 is widely expressed and functions both as a full-length kinase and in a truncated form generated by caspase cleavage during apoptosis, with distinct actions in cell survival and programmed cell death[2][4][9]. PAK2 is implicated in cancer biology (including growth and migration), neurodevelopment, and cardiovascular protection. It is considered a potential therapeutic target, though selective inhibitors are in research stages rather than clinical use[3][1][4].
- Other names
- p21-activated kinase 2P21 (RAC1) activated kinase 2Protein kinase PAK2PAK-2
02
Mechanism of action
Small molecule inhibition of kinase activity (blocks phosphorylation of downstream targets) Modulation of RHO GTPase signaling pathways Interference with apoptotic and survival signaling processes
03
Biological functions
Cytoskeleton regulationCell motilityCell cycle progressionApoptosisCell proliferationCell survivalSignal transductionRegulation of cell adhesion
04
Disease associations
CancerCardiovascular disease (specifically heart failure and cardioprotection)Neurodevelopmental disordersApoptosis-related diseases
05
Safety considerations
Potential disruption of cell survival and apoptosis balance, leading to unwanted cell death or survivalPossible off-target effects due to high sequence similarity to other PAK isoforms (e.g., PAK1)Effects on neurodevelopment and myelination if targeted during development[2][4]
06
Interacting drugs
There are no widely approved small molecule drugs clinically targeting PAK2 specifically, but various pan-PAK inhibitors (e.g., IPA-3, FRAX1036) are reported in the research literature as PAK family inhibitors[1]. Most current agents lack clinical selectivity for PAK2.
07
Biomarkers
Phosphorylation status of PAK2 (notably at Ser20)Cleaved (caspase-activated) PAK2 fragment ("PAK-2p34") in apoptosis
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