Tissue Selective E3 Ligase-based Degraders
The efficacy and selectivity of protein degrader drugs depend on their affinity to the target protein but also on the type of E3 ubiquitin ligase (E3) that is recruited to trigger proteasomal degradation. The arsenal of E3s that can be hijacked for targeted protein degradation (TPD) is still largely unexplored. Only about 2% of the more than 600 E3 ligases have been utilized to date. Exploiting additional E3 ligases that are selectively expressed in specific tissues or cell types, can broaden the applicability of TPD as a therapeutic modality.
Topics: Novel Therapeutics