10 minute read
Jan. 18, 2024

Beyond KRAS(G12C): KRAS Roundup Part II

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While KRAS(G12C) has been the most readily targeted form of KRAS thanks to its reactive cysteine residue, other mutations such as KRAS(G12D) make up the majority of KRAS-mutated cancers. 

Selective inhibition of KRAS(G12D) and other KRAS-mutant proteins is challenging in part due to the requirements of inhibitors to bind with strong enough affinity in the absence of the cysteines, and also in part due to differences in dynamics of transition between KRAS states (GDP-bound vs. GTP-bound).

In this roundup, we highlight 12 inhibitors, degraders, and other molecules that reflect progress in overcoming this challenge, including some of the first clinical candidates targeting non-KRAS(G12C)-mutant tumors, and why these molecules are notable.

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