'Molecular glue' stabilizes protein that inhibits development of non–small cell lung cancer and uterine cancer
Protein phosphatase 2A plays a central role in controlling many cell signaling pathways, which are frequently disrupted during tumor development and growth.
Molecular glue RPT04402 stabilizes tumor-suppressive protein PP2A, which inhibits development of non-small cell lung cancer and uterine cancer. This protein phosphatase 2A requires three proteins to bind for proper function and tumor suppression. When PP2A fails to assemble, it is common in lung, uterine, prostate and liver cancer.
University of Michigan researchers found that targeting PP2A using RPT04402 can help treat non-small cell lung cancers with KRAS mutations, which are present in 30% of cases. Combining adagrasib or trametinib with RPT04402 delayed resistance and increased treatment effectiveness in mouse models. The team plans to start clinical trials to test this combination in various cancer types.
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