標的タンパク質分解誘導剤の創薬

抄録

Targeted Protein Degradation (TPD) is an emerging technology in the pharmaceutical industry. Heterobifunctional degraders, known as proteolysis-targeting chimeras (PROTACs), offer an attractive and novel modality. These degraders consist of a Protein of Interest (POI) binder and a binder that recruits E3 ubiquitin ligase, which are joined by a linker. They effectively hijack the ubiquitin-proteasome system, leading to proteolysis of POI.

This novel approach of targeted proteolysis holds significant promise as a therapeutic strategy to regulate protein levels in previously “undruggable” targets, including proteins lacking enzymatic activity or proteins having scaffold function.

In this session, we will introduce a novel therapeutic strategy for the cancer-immunotherapy by combining IRAK-M (interleukin 1 receptor associated kinase 3) silent binder and targeted protein degradation technology that shifts the balance between tolerance and immunity by releasing immunosuppressive activity, leading to a more favorable tumor microenvironment to enhance host immunity.