Article

Suppression of NRF2-dependent cancer growth by a covalent allosteric molecular glue

2024-10-05

Abstract excerpt

The NRF2 transcription factor is constitutively active in cancer where it functions to maintain oxidative homeostasis and reprogram cellular metabolism. NRF2-active tumors exhibit NRF2-dependency and resistance to chemo/radiotherapy. Here we characterize VVD-065, a first-in-class NRF2 inhibitor that acts via an unprecedented allosteric molecular glue mechanism. In the absence of stress or mutation, NRF2 is rapidly...

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Literature Corpus work: c02f93b9-1515-534e-9e91-c28793d28a8a
DOI: 10.1101/2024.10.04.616592

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