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Sep. 18, 2021

RM-018: A KRAS(G12C)ON-cyclophilin A Tri-Complex Inhibitor

RM-018

KRAS(G12C)ON-cyclophilin A tri-complex inh. overcomes KRAS resist. mut. in PDX model natural product related (sanglifehrin); undiscl. Cancer Discov., Apr. 6, 2021 Revolution Medicines, Redwood City, CA

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Drug Hunter Team

The Revolution Medicines KRASG12C inhibitor, RM-018, “glues” KRASG12C to the highly abundant chaperone protein, cyclophilin A, in a tri-complex (KRAS- inhibitor-cyclophilin A) stabilized by protein-protein interactions. KRAS is a driver of cancer cell growth, and mutants including KRASG12C have been hot targets due to the newfound ability to [...]

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