Design and Synthesis of Linker Technologies for Developing Novel Therapeutic Conjugates

The discovery and development of new therapeutic agents has recently moved into a key new area, looking to combine two distinct classes of chemical or biological agents into a single entity. Bringing two different agents together provides the opportunity for synergistic effects, most notably when one of the components acts as a targeting agent and the other interacting with the desired biological system. One of the leading areas for new synergistic therapeutic modalities is Antibody Drug Conjugates (ADCs). The antibody of an ADC is selected or engineered to bind to a tumour cell-specific antigen or to an antigen that is overexpressed on the surface of tumour cells. Thus, the antibody guides the ADC selectively to target tumour cells. Upon binding, the ADC is internalized and the cytotoxic agent is released from the antibody to perform its cell-killing function. Linker technology remains a comparatively underdeveloped aspect of ADCs. This research aims to develop enhanced linker technologies capable of overcoming current shortcomings.