There are two members--FRS2alpha and FRS2beta--in the fibroblast growth factor receptor substrate 2 (FRS2) family of docking/scaffolding adaptor proteins. These proteins function downstream of certain kinds of receptor tyrosine kinases (RTKs) that are important for tumorigenesis. FRS2alpha acts as a control centre for fibroblast growth factor receptor signalling and encourages tumorigenesis, while FRS2beta regulates EGFR signalling negatively, and might have a tumour suppressive role. Therefore, both proteins could be good therapeutic targets for the treatment of cancer. To examine the physiological and pathological roles of FRS2, especially in cancer, and describe their potential value as therapeutic targets. A review of relevant literature. Although it is still difficult to develop small compounds to modify functions of FRS2 adaptor proteins, such compounds may be useful as the next generation of molecular targeting drugs. Combination therapy with RTK-targeting drugs and FRS2-targeting drugs may be useful for cancer treatment in the near future.