The FK506-binding protein (FKBP) family plays a key role in a variety of tumors and is involved in the regulation of important signaling pathways including AKT, NF-κB and p53, which affects cell proliferation, migration, and multiple cell death modes. Here, we summarize the findings that different FKBP family members exhibit dual functions of promoting or inhibiting tumorigenesis in different types of tumors. The expression levels of FKBP family members are closely related to the prognosis of patients, thus might be used as potential diagnostic and prognostic biomarkers. In the future, it is necessary to combine single-cell sequencing to resolve the spatial distribution of FKBP isoforms, develop clinical validation to promote the translation from molecular mechanism to precision therapy.