化学
结合
药品
抗体-药物偶联物
组合化学
立体化学
抗体
计算生物学
生物化学
药理学
单克隆抗体
免疫学
医学
数学分析
数学
生物
作者
C.-J. Luo,A. L. Ren,Zixuan Jin,Jianxin Zhang,Wei Shi,Yue Zeng,Zhao‐Jun Liu,Mengru Lu,Yajing Hou,Feng Tang,Wei Huang
标识
DOI:10.1016/j.bmc.2024.117828
摘要
The approval of Trodelvy® validates TROP2 as a druggable but challenging target for antibody-drug conjugates (ADCs) to treat metastatic triple-negative breast cancer (mTNBC). Here, based on the TROP2-targeted antibody sacituzumab, we designed and developed several site-specific ADC candidates, which employ MMAE (monomethyl auristatin E) as the toxin, via IgG glycoengineering or affinity-directed traceless conjugation. Systematic evaluation of these site-specific ADCs in homogeneity, hydrophilicity, stability, and antitumor efficiency was conducted. The results indicate that the site-specific ADCs gsADC 3b made from one-step glycoengineering exhibit good aggregation stability and in vivo efficacy, providing a new format of ADCs that target TROP2.
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