Potent Inhibitor of Human Trypsins from the Aeruginosin Family of Natural Products.

ABSTRACT: Serine proteases regulate many physiological processes and play a key role in a variety of cancers. Aeruginosins are a family of natural products produced by cyanobacteria that exhibit pronounced structural diversity and potent serine protease inhibition. Here, we sequenced the complete genome of Nodularia sphaerocarpa UHCC 0038 and identified the 43.7 kb suomilide biosynthetic gene cluster. Bioinformatic analysis demonstrated that suomilide belongs to the aeruginosin family of natural products. We identified 103 complete aeruginosin biosynthetic gene clusters from 12 cyanobacterial genera and showed that they encode an unexpected chemical diversity. Surprisingly, purified suomilide inhibited human trypsin-2 and -3, with IC₅₀ values of 4.7 and 11.5 nM, respectively, while

SUBMITTER: Ahmed MN 

PROVIDER: S-EPMC8609519 | biostudies-literature | 2021 Nov

REPOSITORIES: biostudies-literature