In summary, gossypol is a dual inhibitor of MDM2 and VEGF that disrupts the molecular interaction between MDM2 protein and VEGF mRNA, induces MDM2 self-ubiquitination and degradation, decreases VEGF mRNA stability and protein translation simultaneously, and therefore exerts anti-cancer effects through apoptotic and anti-angiogenesis pathways in human breast cancer in vitro and in vivo, regardless of the p53 status of the cancer cells. This evidence concerns the gene VEGFA and cancer.