Development of target protein-selective degradation inducer for protein knockdown
Development of target protein-selective degradation inducer for protein knockdown
复制标题
DOI：
10.1016/j.bmc.2011.03.057
复制
发表时间：
2011-05-15
影响因子：
3.5
通讯作者：
Hashimoto, Yuichi
中科院分区：
文献类型：
--
作者：
Itoh, Yukihiro;Ishikawa, Minoru;Hashimoto, Yuichi
我们以前的技术，用于诱导选择性降解的目标蛋白与酯型SNIPER（特异性和非遗传性抑制剂-的-apps-依赖性蛋白质擦除器）降解的目标蛋白和IAP。在这里，我们设计了一种小分子酰胺型SNIPER来克服这个问题。作为概念的证明，我们合成和生物学评价酰胺型SNIPER诱导细胞视黄酸结合蛋白II（CRABP-II）的选择性降解，但不是IAP。这种小分子的酰胺型SNIPER诱导靶蛋白选择性降解而不影响IAP，应该是研究活细胞中靶蛋白生物学作用的有效工具。(C)2011爱思唯尔有限公司保留所有权利。
Our previous technique for inducing selective degradation of target proteins with ester-type SNIPER (Specific and Nongenetic Inhibitor-of-apoptosis-proteins (IAPs)-dependent Protein ERaser) degrades both the target proteins and IAPs. Here, we designed a small-molecular amide-type SNIPER to overcome this issue. As proof of concept, we synthesized and biologically evaluated an amide-type SNIPER which induces selective degradation of cellular retinoic acid binding protein II (CRABP-II), but not IAPs. Such small-molecular, amide-type SNIPERs that induce target protein-selective degradation without affecting IAPs should be effective tools to study the biological roles of target proteins in living cells. (C) 2011 Elsevier Ltd. All rights reserved.