Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 23, Issue 13, Pages 3884-3886Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2013.04.066
Keywords
Spongiacidin C; Pyrrole alkaloid; Stylissa massa; USP7 inhibitor
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Funding
- Ministry of Education, Culture, Sports, Science and Technology of Japan [22310138, 22406001]
- Naito Foundation
- Astellas Foundation for Research on Metabolic Disorders
- Uehara Memorial Foundation
- Grants-in-Aid for Scientific Research [22310138, 25108719, 22406001, 25293025] Funding Source: KAKEN
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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 mu M among several USP family members tested. (c) 2013 Elsevier Ltd. All rights reserved.
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