Target intelligence / Profile preview

Phosphoinositide 3-kinase–protein kinase B signaling pathway (PI3K–AKT signaling pathway)

Target
PI3K–AKT signaling pathway
Molecular classification
Other (signaling pathway)
01

Overview

The PI3K–AKT signaling pathway is a critical intracellular signaling cascade involved in regulating diverse cellular processes such as cell proliferation, survival, growth, metabolism, and apoptosis suppression[1][2][3][4][5][6]. Activation of this pathway occurs via various cell surface receptors, including receptor tyrosine kinases, which recruit and activate PI3K, leading to the generation of PIP3 and subsequent activation of AKT. Activated AKT then phosphorylates a wide array of downstream targets that promote cell growth and survival while inhibiting apoptosis. Disruption or hyperactivation of this pathway is frequently observed in cancer and several other diseases, making individual components like PI3K or AKT attractive therapeutic targets[1][2][3][4][5][6][7]. However, the PI3K–AKT signaling itself is not a single molecule or protein but a multi-component signaling axis. Note: The PI3K–AKT signaling pathway is not a molecule or receptor but an intracellular signaling pathway. Individual components (e.g., PI3K catalytic subunit alpha [PIK3CA], AKT1) can be considered therapeutic targets. This entry is marked as "is_incorrect: true" for cases requiring a single molecular target rather than a pathway.

Other names
PI3K/AKT pathwayPI3K-AKT-mTOR pathway
02

Mechanism of action

Inhibition of PI3K enzymatic activity; Inhibition of AKT serine/threonine kinase; Inhibition of mTOR activity downstream

03

Biological functions

Signal transductionCell cycle regulationCell proliferationCell growthCell survivalApoptosis inhibitionAngiogenesisMetabolism
04

Disease associations

CancerDiabetesCardiovascular diseaseNeurodegenerative diseaseInflammation
05

Safety considerations

HyperglycemiaImmunosuppression/infection riskDermatologic toxicitiesGastrointestinal side effectsMetabolic disturbances
06

Interacting drugs

Everolimus (downstream mTOR inhibitor)

7 more in the full profile.

07

Biomarkers

Phosphorylated AKT (p-AKT)PIK3CA mutationPTEN loss/mutationAKT1 (E17K) mutation

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