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. 2025 Jun;31(6):498-500.
doi: 10.1016/j.molmed.2025.03.007. Epub 2025 Apr 3.

Targeting the Yin and Yang of KRASG12C

Christos Adamopoulos  1 , Kostas A Papavassiliou  2 , Athanasios G Papavassiliou  3
Affiliations

Targeting the Yin and Yang of KRASG12C

Christos Adamopoulos et al. Trends Mol Med. 2025 Jun.

Abstract

In a recent study in Cancer Discovery, Maciag et al. introduce BBO-8520, a novel inhibitor targeting both the active and inactive states of KRASG12C. This dual inhibition shows superior target engagement and prolonged tumor suppression, offering a compelling strategy to overcome resistance development and improve outcomes in KRASG12C-mutant cancers.

Keywords: KRAS(G12C); MAPK signaling; covalent inhibitor; dual inhibition.

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Conflict of interest statement

Declaration of interests The authors declare no conflicts of interest.

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