This presentation will focus on the development of a novel two-step conjugation approach that combines the site specificity of the transglutaminase reaction with the reliability of the well-known Diels-Alder reaction. Attendees will gain insight into:

• Re-purposing the maleimides for conjugation to antibodies. A different application that specifically conjugates via cycloaddition reaction versus conjugation to interchain disulfides or engineered cysteines.
• Design and synthesis of diene-containing linkers for site specific transglutaminase conjugation. Modulation of the reactivity of the dienes for conjugation of two different payloads to generate dual-payload ADCs.
• Evaluation of the in vitro and in vivo activity of the ADCs generated via this transglutaminase – Diels-Alder approach, including the assessment of their stability.
• Highlight the importance of collaborations with Contract Research Organizations (CROs) for discovering and developing novel linker and conjugation technologies