Site-Specific Conjugation to Cys-Engineered THIOMAB™ …
Antibodies bearing engineered cysteine residues (termed THIOMAB™ antibodies) enable the site-selective attachment of a drug, label or other payload for specific delivery to certain tissues (e.g., tumors). This Chapter describes detailed methods we have developed and optimized for the conjugation, pu …
从头学习抗体药物偶联（ADC）（第四期：ADC药物关键要素梳理 …
最出名的便是基因泰克的THIOMAB技术了，他们采用基因工程技术在抗体特定位置处插入半胱氨酸残基, 然后将半胱氨酸上的巯基和药物分子偶联,合成了位点专一的抗体药物偶联物, 其中药物抗体比为2的产物高达92.1%。这种定点偶联的方式既不会干扰免疫球蛋白折叠 ...
ADC的四大经典定点偶联技术 - 健康界
2022年12月6日 · thiomab技术是第一个对天然氨基酸进行修饰，将未配对的半胱氨酸进行位点特异性的方法。 该方法将半胱氨酸残基插入抗体重链(HC)或轻链(LC)的不同位置进行偶联（图1）。
A Platform for the Generation of Site-Specific Antibody–Drug …
2020年7月22日 · THIOMAB antibody technol. utilizes cysteine residues engineered onto an antibody to allow for site-specific conjugation. The technol. has enabled the exploration of different attachment sites on the antibody in combination with small mols., peptides, or proteins to yield antibody conjugates with unique properties.
Use of a next generation maleimide in combination with THIOMAB ...
Herein we demonstrate that conjugation of a next generation maleimide (NGM) to engineered cysteines in a THIOMAB™ antibody delivers a THIOMAB™ antibody-drug conjugate (TDC) with a drug loading of ca. 2. This TDC is highly stable in blood serum conditions, selective and potent towards HER2 expressing cell lines and meets the current criteria ...
双载荷ADC的构建思路| Antibody-drug conjugates with dual …
2023年11月21日 · 这里介绍一下定点偶联技术，Thiomab技术：Thiomab技术最早由Genentech公司的 Junutula等报道, 采用基因工程技术在曲妥珠单抗(trastuzumab)的轻链V110C和重链A114C特定位置处插入半胱氨酸残基, 然后将半胱氨酸上的巯基和单甲基auristatinE (MMAE) 偶联，合成了位点专一的抗体− ...
ADC| 从头解析Genetech的THIOMAB定点偶联ADC技术平台 - 知乎
thiomab™技术通过两大突破性创新解决了这些痛点。首先是"精准制导"的偶联策略：研究人员通过基因工程技术，在抗体特定位点（如轻链第205位半胱氨酸，lc-v205c）引入反应性半胱氨酸残基，实现了dar严格为2的高度均一性。
初识抗体偶联药物——笔记整理版 - 雪球
2019年12月17日 · Thiomab技术：Thiomab技术最早由Genentech公司的 Junutula等报道, 采用基因工程技术在曲妥珠单抗(trastuzumab)的轻链V110C和重链A114C特定位置处插入半胱氨酸残基, 然后将半胱氨酸上的巯基和单甲基auristatinE (MMAE) 偶联，合成了位点专一的抗体−药物偶联物，其中药抗比为2 ...
Determination of the decapping efficiency of THIOMAB™ …
2024年12月17日 · The site-specific antibody-drug conjugates (ADCs), particularly those utilizing the engineered cysteine in Fc fragments of mAbs (THIOMAB™ antibodies), have emerged as a novel class of biotherapeutics for cancer treatment. The engineered cysteine residues in these antibodies are capped by cysteine or …
A homogeneous high-DAR antibody-drug conjugate platform …
2022年1月28日 · Herein, we describe the development of a novel bioconjugation platform combining cysteine-engineered (THIOMAB) antibodies and recombinant XTEN polypeptides for the unprecedented generation of homogeneous, stable "TXCs" with DAR of up to 18.