Diarylcarbonates are a new class of deubiquitinating enzyme inhibitor.
Diarylcarbonates are a new class of deubiquitinating enzyme inhibitor.
复制标题
二芳基碳酸酯是一类新型去泛素化酶抑制剂。
DOI：
10.1016/j.bmcl.2018.11.055
复制
发表时间：
2019
影响因子：
2.7
通讯作者：
Hedstrom,Lizbeth
中科院分区：
文献类型：
--
作者：
Long,MarcusJC;Lawson,AnnP;Baggio,Rick;Qian,Yu;Rozhansky,Lior;Fasci,Domenico;ElOualid,Farid;Weerapana,Eranthie;Hedstrom,Lizbeth
酪氨酸蛋白激酶、蛋白水解酶和磷酸酶的混合抑制剂是探索调节途径和稳定裂解产物的有用试剂，也是设计更具选择性的药物的起点。泛素化调节许多关键的细胞过程，而去泛素酶的混杂抑制物(DUBS)也同样有价值。目前可用的混杂DUB抑制剂是能够使蛋白质交联的高活性亲电化合物。在这里，我们介绍了二芳基碳酸酯作为一类新的混杂复制抑制剂，它不具有与以前报道的化合物相关的责任。二芳基碳酸酯稳定细胞和裂解物中的高分子量泛素库。它们还诱导了与Dub抑制相关的细胞表型，证明了它们在泛素发现中的作用。二芳基碳酸盐也可能是开发特定DUB抑制剂的有用支架。
Promiscuous inhibitors of tyrosine protein kinases, proteases and phosphatases are useful reagents for probing regulatory pathways and stabilizing lysates as well as starting points for the design of more selective agents. Ubiquitination regulates many critical cellular processes, and promiscuous inhibitors of deubiquitinases (DUBs) would be similarly valuable. The currently available promiscuous DUB inhibitors are highly reactive electrophilic compounds that can crosslink proteins. Herein we introduce diarylcarbonate esters as a novel class of promiscuous DUB inhibitors that do not have the liabilities associated with the previously reported compounds. Diarylcarbonates stabilize the high molecular weight ubiquitin pools in cells and lysates. They also elicit cellular phenotypes associated with DUB inhibition, demonstrating their utility in ubiquitin discovery. Diarylcarbonates may also be a useful scaffold for the development of specific DUB inhibitors.
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DOI：
10.1016/j.bbamcr.2012.05.014
发表时间：
2012-11
期刊：
Biochimica et biophysica acta
影响因子：
--
作者：
Kramer HB;Nicholson B;Kessler BM;Altun M
通讯作者：
Altun M
影响因子：
3.9
作者：
Colland, Frederic
通讯作者：
Colland, Frederic
DOI：
10.1016/j.bbrc.2004.05.098
发表时间：
2004-07-09
影响因子：
3.1
作者：
Li, ZM;Melandri, F;Figueiredo-Pereira, ME
通讯作者：
Figueiredo-Pereira, ME
影响因子：
8.6
作者：
Lamberto I;Liu X;Seo HS;Schauer NJ;Iacob RE;Hu W;Das D;Mikhailova T;Weisberg EL;Engen JR;Anderson KC;Chauhan D;Dhe-Paganon S;Buhrlage SJ
通讯作者：
Buhrlage SJ
影响因子：
11.2
作者：
Lawson AP;Long MJC;Coffey RT;Qian Y;Weerapana E;El Oualid F;Hedstrom L
通讯作者：
Hedstrom L