USP7, a deubiquitylating enzyme hydrolyzing the isopeptide bond at the C-terminus of ubiquitin, is an emerging cancer target. We isolated spongiacidin C from the marine sponge Stylissa massa as the first USP7 inhibitor from a natural source. This compound inhibited USP7 most strongly with an IC50 of 3.8 μM among several USP family members tested.

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doi.org/10.1016/j.bmcl.2013.04.066
Bioorganic & Medicinal Chemistry Letters
Staff publications

Yamaguchi, Michitaka, Miyazaki, Mitsue, Kodrasov, Matthew P., Rotinsulu, Henki, Losung, Fitje, Mangindaan, Remy E.P., … Tsukamoto, Sachiko. (2013). Spongiacidin C, a pyrrole alkaloid from the marine sponge Stylissa massa, functions as a USP7 inhibitor. Bioorganic & Medicinal Chemistry Letters, 23(13), 3884–3886. doi:10.1016/j.bmcl.2013.04.066