Validating matrix metalloproteinases as drug targets and anti-targets for cancer therapy

Christopher M Overall, Oded Kleifeld

Research output: Contribution to journalArticleResearchpeer-review

1025 Citations (Scopus)


The matrix metalloproteinases (MMPs) mediate homeostasis of the extracellular environment. They have multiple signalling activities that are commonly altered during tumorigenesis and that might serve as intervention points for anticancer drugs. However, there are many criteria to consider in validating MMPs as drug targets and for the development of MMP inhibitors. The inhibition of some MMPs could have pro-tumorigenic effects (making them anti-targets), counterbalancing the benefits of target inhibition. These effects might partially account for the failure of MMP inhibitors in clinical trials. What are the major challenges in MMP target validation and MMP-inhibitor-drug development?
Original languageEnglish
Pages (from-to)227 - 239
Number of pages13
JournalNature Reviews Cancer
Issue number3
Publication statusPublished - 2006
Externally publishedYes

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