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Genesis Drug Discovery & Development
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Chemistry

Bioconjugation

Conjugation methods are crucial for the successful construction of an ADC. It can influence the drug-to-antibody ratio (DAR), stability, PK, therapeutic index, as well as other properties.

  • Conventional cysteine conjugation: reduction of interchain disulfides followed by conjugation to electrophilic linker payloads (e.g., maleimide, haloacetyl)
  • Site-specific cysteine conjugation: deprotection of mutant cysteine followed by conjugation to linker payloads
  • Lysine conjugation: conjugation to lysine residues via activated ester-containing linker payloadÂ