“Epidermal growth factor receptor (EGFR) is a member of the ErbB family of proteins and are involved in downstream signal transduction, plays prominent roles in cell growth regulation, proliferation, and the differentiation of many cell types. They are correlated with the stage and severity of cancer. Therefore, EGFRs are targeted proteins for the design of new drugs to treat cancers that overexpress these proteins. Currently, several bioactive natural extracts are being studied for therapeutic purposes.
Cannabis has been reported in many studies to have beneficial medicinal effects, such as anti-inflammatory, analgesic, antibacterial, and anti-inflammatory effects, and antitumor activity. However, it is unclear whether cannabinoids reduce intracellular signaling by inhibiting tyrosine kinase phosphorylation. In this study, cannabinoids (CBD, CBG, and CBN) were simulated for binding to the EGFR-intracellular domain to evaluate the binding energy and binding mode based on molecular docking simulation.
The results showed that the binding site was almost always located at the kinase active site. In addition, the compounds were tested for binding affinity and demonstrated their ability to inhibit kinase enzymes. Furthermore, the compounds potently inhibited cellular survival and apoptosis induction in either of the EGFR-overexpressing cell lines.”
https://pubmed.ncbi.nlm.nih.gov/36568260/
“Cannabinoids reduced cell viability in EGFR-positive cells A431 and A549 by decreasing the tyrosine-kinase phosphorylation activity of EGFR.•
In silico analysis shows that cannabinoids bind to the active site of the EGFR-tyrosine kinase by the hydrophobic interaction and hydrogen bonding.•
CBD and CBG significantly induce cancer cells apoptosis in EGFR-positive cell A431.•
The consistent findings suggested that CBD and CBG could be developed as natural tumor-targeting agents for EGFR-positive cancers.
These findings demonstrate that the cannabinoids could be transformed into unique natural compounds for use in the development of anti-EGFR-positive cancer therapies.”
https://www.sciencedirect.com/science/article/pii/S2590257122000529?via%3Dihub