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Target intelligence / Profile preview
Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha E545K mutant (PIK3CA E545K)
- Target
- PIK3CA E545K
- Molecular classification
- Enzyme, Kinase, PI3K, Mutant protein
01
Overview
PIK3CA E545K is an oncogenic hotspot mutation in the PIK3CA gene, encoding the p110α catalytic subunit of PI3K. This mutation, a glutamic acid to lysine substitution at position 545, leads to constitutive activation of PI3K signaling, promoting cell growth, survival, and invasion. It is implicated in various cancers, including breast, colorectal, glioblastoma, head and neck, and cervical cancers, and may contribute to therapy resistance. Targeted therapies are under investigation.
- Other names
- PI3K p110alpha E545KPIK3CA exon 9 mutationE545K PIK3CA
02
Mechanism of action
PI3K inhibition (investigational)
03
Biological functions
Signal transductionCell proliferationCell survivalCell growthCell invasionPhospholipid kinase activity
04
Disease associations
CancerDrug resistance
05
Safety considerations
Potential for off-target effects of PI3K inhibitorsTherapy resistanceLimited clinical data for targeted therapies specific to E545K
06
Interacting drugs
STX-478
2 more in the full profile.
07
Biomarkers
PIK3CA E545K mutation statusPIK3CA mutations
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