用于均相抗体药物偶联的可酸裂解的硫代马来酰亚胺酸连接子。
Acid-cleavable thiomaleamic acid linker for homogeneous antibody-drug conjugation.
机构信息
Department of Chemistry, University College London, 20 Gordon Street, London, WC1H 0AJ, UK.
出版信息
Chem Commun (Camb). 2013 Sep 25;49(74):8187-9. doi: 10.1039/c3cc45220d.
Abstract
In this communication we describe a novel acid-cleavable linker strategy for antibody-drug conjugation. Functional disulfide bridging of the single interchain disulfide bond of a trastuzumab Fab fragment yields a homogeneous antibody-drug conjugate bearing a thiomaleamic acid linker. This linker is stable at physiological pH and temperature, but quantitatively cleaves at lysosomal pH to release the drug payload.
摘要
在本通讯中，我们描述了一种用于抗体药物偶联物的新型酸可裂解连接子策略。曲妥珠单抗 Fab 片段的单个链间二硫键的功能二硫键桥接生成了一种带有硫代马来酰亚胺酸连接子的均一抗体药物偶联物。该连接子在生理 pH 和温度下稳定，但在溶酶体 pH 下定量裂解，释放药物有效载荷。
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