用于谷胱甘肽触发肿瘤响应性药物释放的二硫化物生物共轭物。
Bis-sulfide bioconjugates for glutathione triggered tumor responsive drug release.
作者信息
Wang Tao, Ng David Y W, Wu Yuzhou, Thomas Jessica, TamTran Thuy, Weil Tanja
机构信息
Institute of Organic Chemistry III, University of Ulm, Albert-Einstein-Allee 11, Ulm, Germany.
出版信息
Chem Commun (Camb). 2014 Feb 4;50(9):1116-8. doi: 10.1039/c3cc47003b.
The reaction of bis-sulfone conjugation reagents with disulfide bonds allows the site-specific modification of various peptides and proteins. Herein, we present the intracellular disintegration of bis-sulfide containing somatostatin bioconjugates under controlled, tumor-relevant glutathione levels. GSH responsive release is demonstrated, which offers high potential for designing tumor responsive therapeutics.
双砜共轭试剂与二硫键的反应能够实现对各种肽和蛋白质的位点特异性修饰。在此，我们展示了在可控的、与肿瘤相关的谷胱甘肽水平下，含双硫键的生长抑素生物共轭物在细胞内的分解。已证实其对谷胱甘肽的响应性释放，这为设计肿瘤响应性治疗药物提供了巨大潜力。
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