通过 RAFT 聚合合成用于蛋白质偶联的半封端马来酰亚胺聚（PEG）
Synthesis of semitelechelic maleimide poly(PEGA) for protein conjugation by RAFT polymerization.
机构信息
Department of Chemistry and Biochemistry and the California NanoSystems Institute, University of California, Los Angeles, 607 Charles E. Young Drive East, Los Angeles, California 90095-1569, USA.
出版信息
Biomacromolecules. 2009 Jul 13;10(7):1777-81. doi: 10.1021/bm9001987. Epub 2009 Jun 9.
Maleimide end functionalized polymers for site-selective conjugation to free cysteines of proteins were synthesized using reversible addition-fragmentation chain transfer (RAFT) polymerization. A furan-protected maleimide chain transfer agent (CTA) was employed in the RAFT polymerization of poly(ethylene glycol) methyl ether acrylate (PEGA). Gel permeation chromatography (GPC) with laser light scattering detection indicated that 20,000 and 39,000 Da polyPEGA had been made with polydispersity indices of 1.25 and 1.36, respectively. The maleimide group on the polymer chain end was exposed by heating the poly(PEGA)s for 4 h. The deprotection efficiency was estimated to be 80 and 60% for poly(PEGA)(20 kDa) and poly(PEGA)(39 kDa), respectively. Maleimide-poly(PEGA)s were conjugated to V131C T4 lysozyme (T4L), and the resultant polymer-protein conjugates were characterized by size exclusion chromatography and gel electrophoresis.
使用可逆加成-断裂链转移（RAFT）聚合，合成了马来酰亚胺末端功能化聚合物，用于蛋白质游离半胱氨酸的选择性偶联。在聚乙二醇甲醚丙烯酸酯（PEGA）的 RAFT 聚合中，使用了呋喃保护的马来酰亚胺链转移剂（CTA）。凝胶渗透色谱（GPC）与激光光散射检测表明，已经制备了 20,000 和 39,000 Da 的聚 PEGA，其多分散指数分别为 1.25 和 1.36。通过将聚（PEGA）加热 4 小时，暴露聚合物链末端上的马来酰亚胺基团。聚（PEGA）（20 kDa）和聚（PEGA）（39 kDa）的脱保护效率估计分别为 80%和 60%。马来酰亚胺-聚（PEGA）与 V131C T4 溶菌酶（T4L）偶联，所得聚合物-蛋白质缀合物通过尺寸排阻色谱和凝胶电泳进行了表征。
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