Break up the liquid droplets where oncogenic transcription happens
Some cancer-driving proteins gather into droplet-like blobs inside the nucleus to switch genes on. Drugs that dissolve those blobs might switch the cancer programme off.
Transcriptional condensates concentrate MYC, fusion oncoproteins, mediator complex and RNA polymerase at super-enhancers. Certain drugs, including some antineoplastics, concentrate selectively in condensates, and condensate-modulating chemotypes have been reported. A dedicated screen using condensate-specific reporters (optoDroplet or in vitro reconstitution with labelled scaffolds) could identify compounds that selectively dissolve oncogenic condensates while sparing normal ones.
- The undruggable drivers · The proteins that drive most cancers, such as MYC, mutant p53 and most RAS variants, still have no good drug.
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not linked directly; found by shared links- PersonBradley E. Bernstein
Shares Broad Institute of MIT and Harvard, Epigenetic drugs (HDAC, DNMT, EZH2, IDH, menin, BET).
- IdeaSwitch off an undruggable oncogene permanently with epigenetic editing
Shares Epigenetic drugs (HDAC, DNMT, EZH2, IDH, menin, BET), The undruggable drivers.
- IdeaA precompetitive consortium for the twenty hardest cancer targets
Shares Broad Institute of MIT and Harvard, The undruggable drivers.
- IdeaAn open map of which cancer proteins any drug can stick to
Shares Broad Institute of MIT and Harvard, The undruggable drivers.
- TrialRASolute 302
Shares Dana-Farber Brigham Cancer Center, The undruggable drivers.
- Key paperDefining a Cancer Dependency Map: which genes each cancer cell line cannot live without
Shares Broad Institute of MIT and Harvard, Dana-Farber Brigham Cancer Center, The undruggable drivers.
- IdeaAttack the backup copy when a tumour has lost the original gene
Shares Broad Institute of MIT and Harvard, The undruggable drivers.
- IdeaLet patients themselves donate their records and samples for ultra-rare cancers
Shares Broad Institute of MIT and Harvard, Dana-Farber Brigham Cancer Center.