Marine invertebrates are the rich source of small molecules with unique chemical skeletons and potent bioactivities; however, the major biological activities tested for marine natural products have been mainly limited to the traditional phenotype-oriented bioactivities such as cytotoxicity or antimicrobial activities. Enzyme inhibition is the target-oriented bioactivity and small molecule inhibitors are quite useful for controlling biological processes and understanding complicated biological phenomena. Recently, it has been recognized that the natural products are superior source of small molecule probes useful for the chemical biology. Especially, marine-derived enzyme inhibitors still remain to be fully investigated in spite of their high potentials as a source of unique compounds. In this chapter, selected enzyme inhibitors from marine invertebrates are described.
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