Matrix metalloproteinases (MMPs) are members of zinc-dependent endopeptidases implicated
in a variety of physiological and pathological processes. Over the decades, MMPs have
been studied for their role in cancer progression, migration, and metastasis. As a
result, accumulated evidence of MMPs incriminating role has made them an attractive
therapeutic target. Early generations of broad-spectrum MMP inhibitors exhibited potent
inhibitory activities, which subsequently led to clinical trials. Unexpectedly, these
trials failed to meet the desired goals, mainly due to the lack of efficacy, poor
oral bioavailability, and toxicity. In this review, we discuss the regulatory role
of MMPs in cancer progression, current strategies in targeting MMPs for cancer treatment
including prodrug design and tumor imaging, and therapeutic value of MMPs as biomarkers
in breast, lung, and prostate cancers.