Tissue inhibitors of metalloproteinases (TIMPs) play a key regulatory role in the homeostasis of the extracellular matrix (ECM) by controlling the activity of matrix metalloproteinases (MMPs). Some TIMPs have a second function as well, unrelated to their antiMMP activity, which affects cell proliferation and survival. The role of these inhibitors in cancer has been the subject of extensive investigations that have examined their biological activity in tumor growth, invasion, metastasis and angiogenesis, as well as their potential use in the diagnosis and treatment of human cancer.