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November 8, 2025Open Access

Characterisation of Small-Molecule GCN2 Modulators

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Key Points

This project explores the activation mechanisms of GCN2 by small-molecule inhibitors and their implications for tumour treatment.
Expressed and purified GCN2 from Sf9 cells.
Conducted ADP-Glo kinase assays to evaluate ATP-hydrolysis.
Performed hydrogen-deuterium exchange mass spectrometry to study compound binding and effects.
Dabrafenib and other inhibitors demonstrate a GCN2-dependent activation of the integrated stress response.
Compounds activate GCN2 in a concentration-dependent manner.
Evidence of allosteric effects and binding sites on GCN2 was identified.

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Cite This Study

Neill Graham (2025) studied this question.

synapsesocial.com/papers/692502c987af00ed34ac2572 https://doi.org/10.15132/20000721

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