Marine invertebrates are rich sources of small molecules with unique chemical skeletons and potent bioactivities. Historically, such compounds were discovered mainly through the use of assays for phenotype-oriented activities, such as cytotoxicity or antimicrobial effects. More recently, target-oriented searches for bioactive substances, as exemplified by enzyme inhibitors, have become much more common, given a growing need for small-molecule inhibitors essential for studies of complex processes at the interface of chemistry and biology. In this review, selected enzyme inhibitors from marine invertebrates are presented.
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