Protein Variants | Comment | Organism |
---|---|---|
E545K | a dominant activating mutation of the catalytic subunit PIK3CA that is prevalent in breast cancer and confers resistance to lapatinib, lapatinib effectively inhibits the transactivation of EGFR and HER2 by IGF-I signaling | Homo sapiens |
H1047R | a dominant activating mutation of the catalytic subunit PIK3CA that is prevalent in breast cancer and confers resistance to lapatinib, lapatinib effectively inhibits the transactivation of EGFR and HER2 by IGF-I signaling | Homo sapiens |
additional information | deregulation of the PI3K pathway, either through loss-of-function mutations in PTEN or dominant activating mutations in PIK3CA, leads to lapatinib resistance, which can be effectively reversed by NVP-BEZ235. Constitutive activation of the PI3K pathway decreases sensitivity to trastuzumab and lapatinib, overview | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
NVP-BEZ235 | a mTOR/phosphatidylinositol 3-kinase inhibitor. Effector lapatinib and the PI3K inhibitor NVP-BEZ235 collaborate to suppress the PI3K-AKT-mTOR axis driven by loss-offunction PTEN mutations, overview | Homo sapiens |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
- |
- |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
breast cancer cell | - |
Homo sapiens | - |
BT-474 cell | - |
Homo sapiens | - |
carcinoma cell | - |
Homo sapiens | - |
SK-BR-3 cell | a cell line overexpressing the HER2/c-erb-2 gene product | Homo sapiens | - |
Synonyms | Comment | Organism |
---|---|---|
PI3K | - |
Homo sapiens |