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5 Cards in this Set

  • Front
  • Back

RAS-d

Ras cannot hydrolyze GTP, it's always associated with RAF, to make it you sterically block the gamma phosphate (G12-X amino acid change most often or Glu61-X)

Kras

Most common. G12 is mutational hotspot.

Rigosertib, lonafarnib, and vemurafenib

Rigosertib: Blocks Ras ability to bind to RAF.


Lonafarnib: prevents lipid attachment to Ras (unsuccessful)


Vemurafenib: inhibits downstream effectors

Imatinib/gleevec

Blocks BCR-abl kinase's substrate binding domain

P61B-RafV600E

Resistant to vemurafenib