Targeted protein degradation is an emerging therapeutic modality which has made tremendous progress and attracted massive investment in recent years. This modality is a class of bifunctional small molecules composed of an E3 ligase binder linked to a target protein binding moiety. It offers the possibility to degrade any intracellular target proteins regardless if there is a well-defined binding pocket in the target protein. Therefore, it opens numerous opportunities to drug many previously unreachable targets. However, the molecules tend to be bulky, floppy, greasy, and lack drug likeness properties. Nevertheless, increasing preclinical animal data has demonstrated the desired efficacy. Very recently, the early clinical safety and PK results are encouraging. In this forum our expert panel will share key learnings about this novel modality and discuss strategies to overcome potential challenges ahead.
Sponsored by MassBio's Drug Discovery forum working group.
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