Lighting up the PEGylation agents via the Hantzsch reaction
Lighting up the PEGylation agents via the Hantzsch reaction
复制标题
通过 Hantzsch 反应点亮聚乙二醇化试剂
DOI：
10.1039/c5py01624j
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发表时间：
2016
影响因子：
4.6
通讯作者：
Tao Lei
中科院分区：
文献类型：
--
作者：
Zhang Qingdong;Zhao Yuan;Yang Bin;Fu Changkui;Zhao Lingyun;Wang Xing;Wei Yen;Tao Lei
荧光聚乙二醇化剂已经通过Hantzsch反应容易地合成。与其他方法不同的是，蛋白质反应性基团已经通过固有荧光的Hantzsch酯连接在PEG链末端，以原位产生荧光蛋白质反应性PEG。因此，在与蛋白质缀合后，多功能聚合物不仅可以像正常聚乙二醇化剂那样充当蛋白质的保护伞，而且还可以向蛋白质缀合物引入新的功能以实现多功能蛋白质缀合物。多功能蛋白质缀合物在UV下是直接可见的，并且保留了几乎完整的生物活性，初步表明“老”Hantzsch反应在有机化学之外的其他领域（聚合物化学、化学生物学）中的新应用。
Fluorescent PEGylation agents have been facilely synthesized through the Hantzsch reaction. Different from other methods, a protein reactive group has been linked at the PEG chain ends through a Hantzsch ester, which is inherently fluorescent, to in situ generate fluorescent protein-reactive PEGs. Therefore, after conjugation with a protein, the multifunctional polymers can not only act as a protective umbrella to the protein like normal PEGylation agents, but also introduce new functions to the protein conjugates to achieve multifunctional protein conjugates. The multifunctional protein conjugates are directly visible under UV and retain nearly intact bioactivity, preliminarily suggesting the new application of the ‘old’ Hantzsch reaction in other areas (polymer chemistry, chemical biology) outside organic chemistry.