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Target intelligence / Profile preview
PIK3CA E542K Mutant (PIK3CA E542K)
- Target
- PIK3CA E542K
- Molecular classification
- Enzyme, Kinase, PI3K, Oncogene
01
Overview
The PIK3CA E542K mutant is a gain-of-function mutation in the PIK3CA gene, specifically a glutamic acid to lysine substitution at position 542 in the helical domain of the p110α catalytic subunit of PI3K. This mutation leads to constitutive activation of the PI3K/AKT/mTOR signaling pathway, promoting oncogenic transformation and tumorigenesis. It is found in various cancers, including breast, colon, glioblastoma, ovarian, and bladder cancer, and represents a therapeutic target for precision oncology.
- Other names
- PIK3CA E542KPIK3CA (E542K)PIK3CA exon 9/exon 10 E542Kp110α E542K
02
Mechanism of action
PIK3CA E542K inhibitors specifically bind to and inhibit the mutant form of PI3K, shutting down aberrant signaling pathways that drive cancer cell growth and survival.
03
Biological functions
Cell growthCell proliferationCell survivalCell migrationMetabolismSignal transduction (PI3K/AKT/mTOR pathway)
04
Disease associations
CancerOncogenesis
05
Safety considerations
Potential for off-target effectsDevelopment of resistanceToxicity related to PI3K pathway inhibition
06
Interacting drugs
PI3K inhibitors
2 more in the full profile.
07
Biomarkers
PIK3CA E542K mutation status
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