July 8, 2021 12:00
Date: 8th July at 12:00pm
Title: Targeted protein degradation: genetic determinants and drug discovery opportunities
CSIC Conecta link: https://conectaha.csic.es/b/xav-qie-nky-zmi
Molecular glue degraders have incredible therapeutic potential, particularly considering delivering on the promise of degrading “undruggable” proteins. However, their discovery has thus far been largely serendipitous. We have established a scalable strategy toward glue degrader discovery that is based on chemical screening in cell models where many E3 ligases are functionally impaired. This approach led us to identify novel chemical scaffolds functioning as cyclin K degraders. Collectively, our data outline a versatile and broadly applicable strategy to identify molecular glues at scale and thus empower future drug discovery efforts.