Phosphoinositide 3-kinase catalytic subunit gamma (PI3K p110γ)

PI3K p110γ is the catalytic subunit of the class IB phosphoinositide 3-kinase, encoded by the PIK3CG gene. PI3Kγ forms heterodimers with regulatory subunits p101 or p84, and is uniquely activated downstream of G protein–coupled receptors, integrating signals from Gβγ subunits and Ras to modulate cellular signaling. Its central role in leukocyte migration, inflammation, cardiac function, and cancer progression makes it a key therapeutic target, though safety concerns exist due to its broad involvement in immune and cardiovascular pathways. The complex structure of p110γ enables nuanced regulation and multiple routes for pharmacological inhibition, including ATP-competitive and allosteric mechanisms[1][2][3][4][5][6].

Other names

PI3K gammap110γPI3KCGPIK3CGclass IB PI3K catalytic subunit

ATP-competitive inhibition of the lipid kinase domain; Allosteric inhibition of regulatory subunit interface or kinase domain dynamics (e.g., nanobodies); Modulation of upstream interactions (disruption of Gβγ or Ras binding)