Review Article

ErbB Proteins as Molecular Target of Dietary Phytochemicals in Malignant Diseases

Table 2

Natural molecules which target ErbB proteins.

NameTargetMechanism of actionClinical applications/
in vitro or in vivo experiments
References

Epigallocatechin-3-gallate (EGCG)EGFR
ErbB2
ErbB3
ErbB4
Inhibits the binding of EGF to EGFR followed by inhibition of the signaling pathways
Alters the lipid organization on the plasma membrane (lipid rafts)
Promotes internalization of nonactivated EGFR monomer
Reduces phosphorylation of EGFR
Clinical trial HNSCC;
in vitro experiments: epidermoid carcinoma cell line (A-431)
[84, 85, 166, 167]
QuercetinErbB2
ErbB3
Reduces the expression level of ErbB2 and ErbB3
Reduces phosphorylation of ErbB2 and ErbB3
In vitro experiments: prostate cancer cell lines[168, 169]
CurcuminEGFR
ErbB2
Induces degradation of ErbB2 by ubiquitination
Induces EGFR degradation
In vitro experiments: EGFR in several lung adenocarcinoma cell lines; ErbB2 transfected COS7 cell line[97, 98, 170]
ResveratrolErbB2Downregulates ErbB2 gene
Induces apoptosis
In vitro experiments: SK-BR-3 breast cancer cell lines[171]
ApigeninErbB2
ErbB3
Inhibits ErbB2 autophosphorylation and transphosphorylation
Depletes ErbB2 by polyubiquitination
Inhibits the activity of ErbB2/ErbB3 heterodimer
In vitro experiments: BT-474, SK-BR-3 breast cancer cell lines[172]

HNSCC, squamous cell carcinoma of the head and neck.