Article

Paradoxical Activation of GCN2 by ATP-competitive inhibitors via allosteric activation and autophosphorylation

2024-08-14

Abstract excerpt

Recently it has been found that General Control Non-derepressible 2 (GCN2) can be activated by an array of small molecule ATP-competitive inhibitors, including clinically relevant compounds such as Ponatinib, and compounds specifically designed to be GCN2 inhibitors, such as GCN2iB. Furthermore, we recently showed that GCN2 can be activated in cells by clinically approved small molecule RAF inhibitors. GCN2 is a d...

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Literature Corpus work: baed9bdc-3a3b-563b-b506-2aec894bd152
DOI: 10.1101/2024.08.14.606984

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