Matrix metalloprotease (MMPs) is a class of Zinc ions-dependent proteolytic enzymes that play an important role in the degradation of extracellular matrix (ECM), tissue reconstruction, and regulation of various soluble factors in cells. Closely related to tumorigenesis, invasion and metastasis, MMPs are responsible for occurrence of many malignant tumors. MMPs are also involved in many physiological processes such as embryonic development, angiogenesis and wound healing. Under normal physiological conditions, MMPs and tissue inhibitors of metalloproteinases (TIMP) together regulate ECM turnover and maintain cell stability. MMPs dysregulation can accelerate the degradation of the matrix barrier, or indirectly promote tumor growth, invasion and metastasis through releasing matrix-related growth factors. Therefore, MMPs have become an attractive target for tumor research and anti-tumor drugs development.