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磷化氢介导的一锅法硫醇-烯“点击”制备聚合物-蛋白质共轭物的方法。

Phosphine-mediated one-pot thiol-ene "click" approach to polymer-protein conjugates.

作者信息

Jones Mathew W, Mantovani Giuseppe, Ryan Sinead M, Wang Xuexuan, Brayden David J, Haddleton David M

机构信息

Department of Chemistry, University of Warwick, Coventry, UKCV4 7AL.

出版信息

Chem Commun (Camb). 2009 Sep 21(35):5272-4. doi: 10.1039/b906865a. Epub 2009 Jul 21.

Abstract

We employ water-soluble organic phosphines as key reagents in a one-pot synthetic protocol where a (poly)peptide disulfide bridge is first reduced followed by subsequent reaction of the two thiols in situ with poly(monomethoxy ethylene glycol)(meth)acrylates (p(mPEG)(M)A); we use salmon calcitonin (sCT) as a disulfide bridge-containing peptide, which contains a disulfide bridge-Cys1-Cys7-that can be reduced to give two sulfhydryl units available for thiol functionalisation; bioactivity is retained.

摘要

我们采用水溶性有机膦作为关键试剂,用于一锅合成方案,其中首先还原(聚)肽二硫键,然后使两个硫醇原位与聚(单甲氧基乙二醇)(甲基)丙烯酸酯(p(mPEG)(M)A)反应;我们使用鲑鱼降钙素(sCT)作为含二硫键的肽,其含有二硫键-Cys1-Cys7-,可被还原以产生两个可用于硫醇官能化的巯基单元;生物活性得以保留。

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