부산대학교 도서관

TheRAS proteins play a role in cell differentiation, proliferation, andsurvival. Aberrant RAS signaling has been found to play a role in30% of all cancers. KRAS, a key member of the RAS protein family,is an attractive cancer target, as frequent point mutations in theKRAS gene render the protein constitutively active. A number of attemptshave been made to target aberrant KRAS signaling by identifying smallmolecule compounds that (1) are synthetic lethal to mutant KRAS, (2)block KRAS/GEF interactions, (3) inhibit downstream KRAS effectors,or (4) inhibit the post-translational processing of RAS proteins.In addition, inhibition of novel targets outside the main KRAS signalingpathway, specifically the cell cycle related kinase PLK1, has beenshown have an effect in cells that harbor mutant KRAS. Herein we reviewthe use of various high-throughput screening assays utilized to identifynew small-molecule compounds capable of targeting mutant KRAS-drivencancers. [ABSTRACT FROM AUTHOR]