DIRAS3 mimetic broadly suppresses signaling across KRAS hotspot variants
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A bioRxiv preprint in cancer biology reports that an alpha5 mimetic of DIRAS3, a small GTPase with tumor-suppressor activity, broadly inhibits oncogenic KRAS signaling. The mimetic suppresses MAPK and PI3K pathway signaling driven by diverse KRAS hotspot variants through an inhibitory interface. Immunoprecipitation experiments show it reduces KRAS association with both RAF1 and p110α in G12-mutant and Q61-mutant KRAS. The work also compares the mimetic with RMC-7977, a known KRAS inhibitor, which showed weaker inhibition of Q61 KRAS association with p110α. The findings are at the preprint stage and have not yet undergone peer review; questions of how the inhibitory interface works across variants and how the approach compares with existing inhibitors in clinical settings are still open.
Written by a model from the reports · updated 5 hours ago
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- biorxiv.orgPickDIRAS3 broadly suppresses signaling from diverse oncogenic KRAS hotspot variants through an inhibitory interface
A bioRxiv preprint shows that an alpha5 mimetic of DIRAS3 broadly suppresses MAPK and PI3K signaling driven by diverse KRAS hotspot variants through an inhibitory interface. Immunoprecipitation shows the mimetic reduces KRAS association with RAF1 and p110α in both G12 and Q61 mutants, whereas RMC-7977 shows weaker inhibition of p110α association with Q61 KRAS.
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