Protein-destroying drugs work by hijacking cellular waste-disposal machines. Using a machine that is mostly present in cancer cells would make these drugs safer.
Almost all clinical degraders use cereblon or VHL, both broadly expressed, which limits therapeutic index. Human cells have roughly 600 E3 ligases, many with restricted expression; some are highly enriched in tumour or lineage-specific tissue. The proposal is to map ligase expression across normal and tumour tissue atlases, prioritise tumour-enriched ligases, and develop handles for them, thereby making degraders tissue-selective.
Shares Kymera Therapeutics, Nurix Therapeutics, Drugging the 'undruggable' cancer targets, Proteomics & phosphoproteomics.
Shares Kymera Therapeutics, Nurix Therapeutics, Drugging the 'undruggable' cancer targets, The undruggable drivers.
Shares Kymera Therapeutics, Drugging the 'undruggable' cancer targets, The undruggable drivers, PROTACs & molecular glues (targeted protein degradation).
Shares Kymera Therapeutics, Nurix Therapeutics, The undruggable drivers, PROTACs & molecular glues (targeted protein degradation).
Shares Drugging the 'undruggable' cancer targets, The undruggable drivers, PROTACs & molecular glues (targeted protein degradation).
Shares Drugging the 'undruggable' cancer targets, The undruggable drivers, PROTACs & molecular glues (targeted protein degradation).
Shares Drugging the 'undruggable' cancer targets, The undruggable drivers, PROTACs & molecular glues (targeted protein degradation).
Shares Drugging the 'undruggable' cancer targets, Proteomics & phosphoproteomics, The undruggable drivers.