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Matrix metalloproteinases (MMPs) are a family of zinc-dependent neutral endopeptidases, generally consisting of a single peptide, a propeptide domain, a catalytic domain with a highly conserved zinc-binding site and a haemopexin-like domain, that catalyze the degradation of all components of the extracellular matrix. Multiple studies have shown that MMPs are overexpressed in malignant tumor and involved in the process of tumor growth, invasion and metastasis. Thus, synthetic and naturally occurring MMP inhibitions have been investigated as anti-cancer agents for the treatment of a variety of cancers, which are divided into three pharmacologic categories, including collagen peptidomimetics and nonpeptidomimetics, tetracycline derivatives and bisphosphonates.