Efficient chemical synthesis for the analogue of ubiquitin-based probe Ub-AMC with native bioactivity
Efficient chemical synthesis for the analogue of ubiquitin-based probe Ub-AMC with native bioactivity
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具有天然生物活性的基于泛素的探针 Ub-AMC 类似物的高效化学合成
DOI：
10.1039/c6ra11019c
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发表时间：
2016
期刊：
影响因子：
3.9
通讯作者：
Li Yi-Ming
中科院分区：
文献类型：
--
作者：
Xu Ling;Xu Yang;Qu Qian;Guan Chao-Jian;Chu Guo-Chao;Shi Jing;Li Yi-Ming
通过巯基乙酸甲酯 (MTG) 辅助的一锅连接脱硫方案，有效合成了基于泛素的探针泛素–7-酰胺基-4-甲基香豆素 (Ub–AMC) 的类似物。为了获得更高产率的肽段，在化学合成过程中使用正亮氨酸（Nle）代替蛋氨酸。与天然 Ub-AMC 相比，该类似物表现出折叠良好的二级结构和研究 DUB 酶所需的生物活性。
The analogue of ubiquitin-based probe ubiquitin–7-amido-4-methylcoumarin (Ub–AMC) was efficiently synthesized through a methyl thioglycolate (MTG) assisted one-pot ligation–desulfurization protocol. To obtain peptide segments with higher yield, norleucine (Nle) was used instead of methionine in the chemical synthesis procedure. Compared with native Ub–AMC, the analogue exhibits well-folded secondary structure and desired bioactivity for studying the DUB enzyme.