Target intelligence / Profile preview

Phosphoinositide 3-kinase signaling pathway (PI3K signaling pathway)

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

Overview

The **phosphoinositide 3-kinase signaling pathway** (PI3K pathway) is a fundamental intracellular signal transduction pathway that regulates a wide range of cellular processes, including cell growth, survival, proliferation, metabolism, and apoptosis. It is activated by various receptor classes, notably receptor tyrosine kinases and G protein-coupled receptors, leading to the generation of lipid second messengers that activate downstream effectors such as AKT and mTOR. Aberrant activation or mutation of pathway components is among the most frequent alterations in human cancers, making this pathway a pivotal focus of anticancer drug development. Despite the widespread use of drugs that inhibit nodes within this pathway (such as PI3K, AKT, or mTOR inhibitors), challenges remain in optimizing efficacy and overcoming resistance and side effects. The PI3K signaling pathway is not a single molecular target but a collection of interrelated enzymes and effectors, thus not itself a direct drug target or individual molecule[1][2][3].

Other names
PI3K pathwayPI3K/AKT pathwayphosphoinositide-3-kinase pathwayPI3K-AKT-mTOR pathway
02

Mechanism of action

Inhibition of phosphoinositide 3-kinase catalytic activity Downregulation of AKT signaling Dual inhibition of PI3K/mTOR Suppression of metabolic, proliferative, and cell survival signals

03

Biological functions

Signal transductionCell growthCell proliferationCell survivalApoptosisCell metabolism
04

Disease associations

CancerInflammationOther (tissue overgrowth, metabolic disorders)
05

Safety considerations

HyperglycemiaRashFatigueNausea and vomitingDiarrheaAbnormal liver functionDrug resistanceNarrow therapeutic window[2]
06

Interacting drugs

Alpelisib (BYL-719)

19 more in the full profile.

07

Biomarkers

PIK3CA mutation statusPTEN loss/mutationAKT mutationsPhosphorylated AKT (p-AKT) levels[1][2]

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