Introduction: Cancer immunotherapy has been recently presented as one of the most efficient treatment approaches for many types of cancer. Toll-like receptor 4 (TLR4) upregulation is involved in the proliferation, migration, and metastasis of many tumors. TAK-242 (also known as Resatorvid) is a TLR4 antagonist which specifically binds to the intracellular domain of the receptor and inhibits all TLR4 interplays with its downstream signaling molecules suggesting a new promising anticarcinogenic strategy.
Objectives: The present research aimed to estimate the antitumorigenic effects of TAK-242 on oral squamous cell carcinoma-4 (OSCC-4) cell line.
Methodology: Verification of TLR4 expression in OSCC-4 cells was established using immunocytochemistry to proof the presence of the studied receptor in the cell line. Next, the cytotoxic effect of TAK-242 was evaluated using MTT assay. The sublethal IC50 dose was calculated then apoptotic induction ability of the drug was assessed using Annexin V/PI assay.
Results: In the present research, it was concluded that TLR4 was significantly expressed in OSCC-4 cells. In addition, its inhibitor (TAK-242) halted cell proliferation by inducing apoptosis of OSCC-4 cells.
Conclusions: TAK-242 has a significant anticarcinogenic effect on OSCC-4 cells and could be further studied experimentally.