RASSF1A: A promising target for the diagnosis and treatment of cancer

•RASSF1A is a promising biomarker in the screening, staging and therapeutic management in human malignancies.•Hypermethylated RASSF1A may identify cancer-acquired resistance and develop a novel drug for cancer-related diseases.•RASSF1A inactivation can dysregulate the RAS, Hippo, Wnt and other tumor-related signaling pathways, which potentially results in drug resistance. The Ras association domain family 1 isoform A (RASSF1A), a tumor suppressor, regulates several tumor-related signaling pathways and interferes with diverse cellular processes. RASSF1A is frequently demonstrated to be inactivated by hypermethylation in numerous types of solid cancers. It is also associated with lymph node metastasis, vascular invasion, and chemo-resistance. Therefore, reactivation of RASSF1A may be a viable strategy to block tumor progress and reverse drug resistance. In this review, we have summarized the clinical value of RASSF1A for screening, staging, and therapeutic management of human malignancies. We also highlighted the potential mechanism of RASSF1A in chemo-resistance, which may help identify novel drugs in the future.