Cancer is one of the leading causes of disease and mortality worldwide. As a result, the past two decades of biomedical research have yielded an enormous amount of information on the molecular events that take place during carcinogenesis and the signaling pathways participating in cancer progression. Matrix metalloproteinases (MMPs) consist of a multigene family of zinc-dependent extracellular matrix (ECM) remodeling endopeptidases implicated in pathological processes, such as carcinogenesis. In this regard, their activity plays a pivotal role in tumor growth and the multistep processes of invasion and metastasis, including proteolytic degradation of ECM, alteration of the cell–cell and cell–ECM interactions, migration and angiogenesis. MMPs are therefore amenable to therapeutic intervention by synthetic and natural inhibitors, providing perspectives for future studies.