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Spongiacidin C,a pyrrole alkaloid from the marine sponge Stylissa massa,functions as a USP7 inhibitor |
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| Authors: | Michitaka Yamaguchi Mitsue Miyazaki Matthew P Kodrasov Henki Rotinsulu Fitje Losung Remy EP Mangindaan Nicole J de Voogd Hideyoshi Yokosawa Benjamin Nicholson Sachiko Tsukamoto |
| Institution: | 1. Department of Natural Medicines, Graduate School of Pharmaceutical Sciences, Kumamoto University, Oe-honmachi 5-1, Kumamoto 862-0973, Japan;2. Division of Research and Development, Progenra, Inc., 277 Great Valley Parkway, Malvern, PA 19355, USA;3. Faculty of Agriculture, Universitas Pembangunan Indonesia, Manado 95361, Indonesia;4. Faculty of Fisheries and Marine Science, Sam Ratulangi University, Kampus Bahu, Manado 95115, Indonesia;5. Netherlands Centre for Biodiversity Naturalis, PO Box 9517, 2300 RA Leiden, The Netherlands;6. School of Pharmacy, Aichi Gakuin University, Chikusa-ku, Nagoya 464-8650, Japan |
| Abstract: | 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. |
| Keywords: | Spongiacidin C Pyrrole alkaloid USP7 inhibitor |
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