A key property needed for the effectiveness of CELMoD drugs, a type of protein degrader, has been discovered. Scripps Research Institute scientists have discovered a crucial feature that is necessary for CELMoDs, a promising new class of cancer drugs, to work effectively. CELMoDs are a new class
CELMoDs, or covalent epitope-linked molecules of degradation, are a type of protein degrader that works by targeting specific proteins for degradation in the body. These drugs have the potential to be used in the treatment of a variety of diseases, including cancer and neurodegenerative disorders, by selectively eliminating proteins that are involved in the progression of these conditions.
Scientists now recognize that some cancer drugs, including the best-selling myeloma drug lenalidomide , happen to work by binding to cereblon. They do so in a way that forces the ubiquitin-tagging, and consequent destruction, of key proteins that promote cell division—proteins that couldn’t be targeted easily with traditional drugs.
In the study, Watson spent more than a year devising a recipe for stabilizing cereblon in association with a ubiquitin-system partner protein, in order to image it with low-temperature electron microscopy . In this way, he was able ultimately to resolve the cereblon structure at a near-atomic scale. Watson also imaged the cereblon-partner complex with CELMoD compounds and target proteins.
“Companies have been developing cereblon-binding protein-degradation drugs that they can see are better degraders, but they didn’t know this was because the drugs are better at driving this closed conformation,” Watson says. “So now they know, and they can test their drugs for this key property.”
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