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ARTICLE | Distillery Therapeutics

Small molecule GPX4 degrader for solid tumors

December 22, 2023 6:30 PM UTC

A small molecule that triggers degradation of the ferroptosis repressor GPX4 in cancer cells by activating the tumor-specific E3 ubiquitin ligase TRIM25 could help treat pancreatic cancer and other solid tumors by inducing tumor cell death, and increasing cytotoxic T cell infiltration and immune memory.

Screening of over 4,000 small molecules in a human pancreatic cancer cell line sensitive to ferroptosis using an infrared dye-based quantitative assay to measure GPX4 expression identified 12 compounds that repressed GPX4...

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