Vialinin A is a ubiquitin-specific peptidase inhibitor
Vialinin A is a ubiquitin-specific peptidase inhibitor
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DOI：
10.1016/j.bmcl.2013.05.093
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发表时间：
2013-08-01
影响因子：
2.7
通讯作者：
Yajima, Shunsuke
中科院分区：
文献类型：
--
作者：
Okada, Kiyoshi;Ye, Yue Qi;Yajima, Shunsuke
Vialinin A是从中国蘑菇Thelephora vialis中分离的小分子化合物，其抗炎活性比广泛使用的免疫抑制药物他克莫司（FK 506）更有效。在这里，我们表明，泛素特异性肽酶5/异肽酶T（USP 5/IsoT）是一个目标分子的vialinin A，通过使用珠探针方法确定。在所测试的去泛素化酶中，Vialinin A抑制USP 5/IsoT的肽酶活性，并且还抑制USP 4的酶活性。尽管USP是巯基蛋白酶家族的成员，但对其他巯基蛋白酶如钙蛋白酶和组织蛋白酶没有抑制作用。(C)2013爱思唯尔有限公司保留所有权利。
Vialinin A, a small compound isolated from the Chinese mushroom Thelephora vialis, exhibits more effective anti-inflammatory activity than the widely used immunosuppressive drug tacrolimus (FK506). Here, we show that ubiquitin-specific peptidase 5/isopeptidase T (USP5/IsoT) is a target molecule of vialinin A, identified by using a beads-probe method. Vialinin A inhibited the peptidase activity of USP5/IsoT and also inhibited the enzymatic activities of USP4 among deubiquitinating enzymes tested. Although USPs are a member of thiol protease family, vialinin A exhibited no inhibitions for other thiol proteases, such as calpain and cathepsin. (C) 2013 Elsevier Ltd. All rights reserved.