Target intelligence / Profile preview

Phosphatidylinositol 3-kinase catalytic subunit beta isoform (PI3Kβ)

Target
PI3Kβ
Molecular classification
Enzyme, Kinase, Intracellular signaling molecule, Lipid kinase
01

Overview

Phosphatidylinositol 3-kinase catalytic subunit beta isoform (PI3Kβ, gene symbol PIK3CB) is a class IA phosphoinositide 3-kinase enzyme that phosphorylates phosphatidylinositol (4,5)-bisphosphate to generate phosphatidylinositol (3,4,5)-trisphosphate (PIP3), a key signaling lipid. PI3Kβ acts downstream of various cell surface receptors—including receptor tyrosine kinases, GPCRs, and integrins—and is involved in mediating diverse cellular responses such as growth, proliferation, migration, and survival. While PI3Kβ is ubiquitously expressed, it plays crucial roles in insulin signaling, cardiovascular homeostasis, and inflammation. In cancer, PI3Kβ is especially important in tumors with PTEN loss, as these may become dependent on PI3Kβ for activating the PI3K/Akt pathway. PI3Kβ is an established drug target, with several selective inhibitors under clinical investigation for cancer and other diseases[4][5][7].

Other names
PI3K betaPI3Kβp110βPIK3CB (gene symbol)Phosphatidylinositol 4,5-bisphosphate 3-kinase beta
02

Mechanism of action

Inhibition of PI3Kβ catalytic activity to downregulate PI3K/Akt/mTOR signaling Reduction of phosphatidylinositol (3,4,5)-trisphosphate (PIP3) production Modulation of downstream cell survival and proliferation pathways

03

Biological functions

Signal transductionCell growthCell proliferationCell differentiationApoptosis regulationCellular metabolismInsulin signalingCardiovascular functionImmune modulation
04

Disease associations

CancerCardiovascular diseaseDiabetes mellitusInflammatory disordersOther (e.g., male infertility, based on animal models)
05

Safety considerations

Hyperglycemia (on-target effect in metabolic tissues)Increased risk of infection (from altered immune signaling)Cardiovascular side effects (QT prolongation, arrhythmia potential)Potential for male infertility (based on animal data)
06

Interacting drugs

AZD8186

3 more in the full profile.

07

Biomarkers

PTEN loss (may indicate dependence on PI3Kβ in some cancers)PIK3CB gene alterations (rare)PI3K pathway activation markers (phospho-Akt)

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