Novel Molecular Glue Discovery Platform Unlocks Undruggable Cancer Targets
A scalable platform to discover molecular glue degraders has been developed, identifying the first metabolically activated glue. The approach expands protein degradation targets, enabling selective elimination of previously undruggable cancer-related proteins for therapeutic development. The post Novel Molecular Glue Discovery Platform Unlocks Undruggable Cancer Targets appeared first on GEN -…
Dana-Farber Cancer Institute researchers have developed a new platform for discovering molecular glue degraders, which could help treat previously undruggable cancer targets. The platform works by fixing a subset of E3 ligases to magnetic beads and bathing them in cellular lysate and a library of drug compounds. When a drug binds to an E3 ligase and increases its affinity for a specific protein, it is considered a hit.
Using this method, the team discovered the first molecular glue degrader activated by glutathionylation, a metabolic activation suggesting molecular glues could be more context-dependent than previously thought. This discovery could expand the range of disease-related proteins that can be targeted for elimination via protein degradation, potentially revolutionizing cancer treatment.
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