ARF1 and head and neck squamous cell carcinoma: In this study, our Arf1-targeting γ-dipeptides revealed anticancer activity in HNSCC cells, which may be linked to the blockade of the EGFR-Arf1 axis, suggesting that targeting the EGFR-Arf1 would constitute a feasible innovative strategy to fight against HNSCC and may provide an alternative strategy over currently used chemotherapy tolerance.