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. An undisclosed molecule in their pipeline with a related mechanism, RMC-6291 , has been reported to be orally bioavailable [...]
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Feb. 9, 2022
RM-018: a KRASG12C-Cyclophilin A Glue
RevMed KRASG12C Tricomplex Inhibitor
KRAS(G12C)ON-cyclophilin A tri-complex inh. overcomes KRAS resist. mut. in PDX model natural product related (sanglifehrin); undiscl. RM-018 Revolution Medicines, Redwood City, CA