P21 (RAC1) activated kinase 3 (PAK3)

P21 (RAC1) activated kinase 3 (PAK3) is a member of the Group I p21-activated kinase family of serine/threonine kinases that function as important effectors of the small GTPases CDC42 and RAC1. PAK3 is principally expressed in neuronal cells and is essential for synapse formation, dendritic spine morphogenesis, and synaptic plasticity. Activated by interaction with GTP-bound CDC42 or RAC1, PAK3 undergoes conformational change and autophosphorylation, regulating downstream pathways that control cytoskeletal dynamics, cellular migration, and the cell cycle. Mutations in PAK3 cause nonsyndromic X-linked intellectual disability, and the kinase is implicated in neural development and potentially in certain tumors. Small molecule inhibitors (such as FRAX597) target PAK family members and are being explored for their effects on cancers and neurological diseases, although modulation of PAK3 must be approached cautiously due to risks of perturbing neuronal development and function.

Other names

p21 protein-activated kinase 3p21-activated kinase 3beta-PAKbPAKhPAK3p21 (CDKN1A)-activated kinase 3p21 protein (Cdc42/Rac)-activated kinase 3MRX30MRX47

Inhibition of kinase activity (as with broad-spectrum PAK inhibitors such as FRAX597)