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In the development of ADC/PDC drugs, linker design and optimization are crucial. The stability of the linker-payload needs to be independently assessed within various in vitro biological incubation systems(e.g., plasma, lysosomes, cathepsin B, β-glucuronidase) without coupling to an antibody or peptide at the early screening stage. Maleimide is widely used as a linker for the conjugation of antibodies or peptides due to its rapid reactivity with thiol groups (-SH) under mild conditions. However, challenges emerge when assessing the stability of linker-payloads containing maleimide groups in in vitro biological matrices.
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