Toxicity of antibody drug conjugates (ADCs) is often caused by off-target shedding of therapeutic payloads due to linker instability. Here, the authors demonstrate that site-specific ligase-dependent conjugation of therapeutic payloads to engineered trastuzumab via a ring-opening linker improves stability compared to conventional HER2- targeting ADCs.
- Lei Huang
- Gang Qin
- Biyun Wang