Grassystatins A− C from marine cyanobacteria, potent cathepsin E inhibitors that reduce antigen presentation

…, EA Eksioglu, C Liu, VJ Paul, H Luesch

Index: Kwan, Jason C.; Eksioglu, Erika A.; Liu, Chen; Paul, Valerie J.; Luesch, Hendrik Journal of Medicinal Chemistry, 2009 , vol. 52, # 18 p. 5732 - 5747

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Citation Number: 40

Abstract

In our efforts to explore marine cyanobacteria as a source of novel bioactive compounds, we discovered a statine unit-containing linear decadepsipeptide, grassystatin A (1), which we screened against a diverse set of 59 proteases. We describe the structure determination of 1 and two natural analogues, grassystatins B (2) and C (3), using NMR, MS, and chiral HPLC techniques. Compound 1 selectively inhibited cathepsins D and E with IC50s of 26.5 nM ...