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Missing the Link, Losing the Toxin: Linker Chemistry, not Conjugation Site, Dictates ADC In Vivo Stability and Efficacy

机译：错过了链接，失去了毒素：链接剂化学，不是共轭部位，决定ADC以体内稳定性和功效

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With the advance in site-specific conjugation, homogeneous ADCs are made with better safety profile and higher efficacy. However, enormous effort was spent to find the right conjugation sites in order to obtain stable ADCs. Using engineered transglutaminase, toxins are conjugated to the endogenous glutamine residues of existing mABs without further re-engineering.

机译：随着特定于现场的缀合的前进，具有更好的安全性和更高的疗效，使均匀ADC制成。然而，花费巨大的努力来找到正确的共轭位点，以获得稳定的ADC。使用工程化转谷氨酰胺酶，毒素与现有MAB的内源性谷氨酰胺残留缀合而无需进一步重新设计。

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《PEGS》|2015年||共1页
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Sean Hu; Lisha Allen; Di Zhang; Yi Mi;
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中图分类生物工程学（生物技术）;
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1. Molecular Basis of Valine-Citrulline-PABC Linker Instability in Site-Specific ADCs and Its Mitigation by Linker Design [J] . Dorywalska Magdalena, Dushin Russell, Moine Ludivine, Molecular cancer therapeutics . 2016,第5期

机译：特定位ADC中缬氨酸-瓜氨酸-PABC接头不稳定性的分子基础及其接头设计的缓解
2. Site-specific labeling of an anti-MUC1 antibody: probing the effects of conjugation and linker chemistry on the internalization process [J] . Xu Hongjiao, Gan Lu, Han Ying, RSC Advances . 2019,第4期

机译：抗MUC1抗体的特异性标记：探测缀合和接头化学对内化过程的影响
3. Site-specific labeling of an anti-MUC1 antibody: probing the effects of conjugation and linker chemistry on the internalization process [J] . Hongjiao Xu, Lu Gan, Ying Han, RSC Advances . 2019,第4期

机译：抗MUC1抗体的位点特异性标记：探讨偶联和接头化学作用对内化过程的影响
4. Missing the Link, Losing the Toxin: Linker Chemistry, not Conjugation Site, Dictates ADC In Vivo Stability and Efficacy [C] . Sean Hu, Lisha Allen, Di Zhang, PEGS . 2015

机译：错过了链接，失去了毒素：链接剂化学，不是共轭部位，决定ADC以体内稳定性和功效
5. Generation of site-specific DNA-polypeptide cross-links mediated by Schiff base chemistry: A novel strategy to investigate the cellular pathways that repair DNA-protein cross-link damage. [D] . Kurtz, Andrew James. 2003

机译：由席夫碱化学介导的位点特异性DNA多肽交联的生成：研究修复DNA蛋白质交联损伤的细胞途径的新策略。
6. Impact of linker and conjugation chemistry on antigen binding Fc receptor binding and thermal stability of model antibody-drug conjugates [O] . Mauro Acchione, Hyewon Kwon, Claudia M. Jochheim, 2012

机译：接头和缀合化学对模型抗体-药物缀合物的抗原结合Fc受体结合和热稳定性的影响
7. Molecular Basis of Valine-Citrulline-PABC Linker Instability in Site-Specific ADCs and Its Mitigation by Linker Design [O] . Magdalena Dorywalska, Russell Dushin, Ludivine Moine, 2016

机译：缬氨酸 - 瓜氨酸-PABC接头在特异性ADC中不稳定性的分子基础及其通过接头设计缓解

Missing the Link, Losing the Toxin: Linker Chemistry, not Conjugation Site, Dictates ADC In Vivo Stability and Efficacy

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