曲妥珠单抗金缀合物的合成及对乳腺癌细胞系抗癌活性的体外评价。
Trastuzumab gold-conjugates: synthetic approach and in vitro evaluation of anticancer activities in breast cancer cell lines.
机构信息
Department of Chemistry Brooklyn College, The City University of New York Brooklyn, NY, 11210, USA.
出版信息
Chem Commun (Camb). 2019 Jan 29;55(10):1394-1397. doi: 10.1039/c8cc08769e.
Abstract
We describe the preparation of gold(i)-compounds that are amenable to efficient bioconjugation with monoclonal antibodies via activated ester or maleimide linkers. New Trastuzumab-gold conjugates were synthesized and fully characterized. These bioconjugates are significantly more cytotoxic (sub-micromolar range) to HER2-positive breast cancer cells than the gold complexes and Trastuzumab.
摘要
我们描述了金（i）化合物的制备方法，这些化合物可通过活化酯或马来酰亚胺接头与单克隆抗体进行有效的生物偶联。新的曲妥珠单抗-金缀合物已被合成并进行了全面表征。与金复合物和曲妥珠单抗相比，这些生物缀合物对 HER2 阳性乳腺癌细胞的细胞毒性更强（亚微摩尔范围）。
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