Department of Natural Medicines, Graduate School of Pharmaceutical Sciences, Kumamoto University, Oe-honmachi 5-1, Kumamoto 862-0973, Japan.
Bioorg Med Chem Lett. 2013 Jul 1;23(13):3884-6. doi: 10.1016/j.bmcl.2013.04.066. Epub 2013 May 3.
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.
USP7 是一种去泛素化酶，可水解泛素 C 末端的异肽键，是一个新兴的癌症靶点。我们从海洋海绵 Stylissa massa 中分离到海绵抑素 C，这是首个从天然产物中获得的 USP7 抑制剂。该化合物对 USP7 的抑制作用最强，在测试的几种 USP 家族成员中，IC50 为 3.8 μM。
Zotero 插件