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Colorectal cancer is a public health problem.Approximately 30 to 50 \% ofcolorectal tumors are caused by mutations in the KRAS gene.These mutationsinduce uncontrolled proliferation.To date,There is no approved effectivetreatment for the mutated KRAS oncogene.Farnesyltransferase (FTI) inhibitorsare considered a therapeutic target against the mutated KRASoncogene.Tipifarnib is a farnesyltransferase inhibitor that was analyzed in aPhase II trial.In the present study, the three-dimensional structure offarnesyltransferase complexed with tipifarnib [1SA4] was used as a basis toexploit the characteristics of tipifarnib.A pharmacophore model was generatedbased on the structure using the Asinex (Gold and Platinum Collections)database.A total of 299 molecules were obtained after screening.The 299molecules were anchored to the tipifarnib binding site in thefarnesyltransferase crystal structure for docking analysis.During the moleculardocking process, the pharmacophore that was modeled, and was used as aconstraint to eliminate the molecules that do not satisfy thepharmacophore.Finally, four Hits identified as farnesyltransferase inhibitorsfor biological tests.  Keywords: colorectal cancer, structure-based pharmacophore, moleculardocking, KRAS, farnesyltransferase inhibitors, Virtual Screening.

In silico Identification of tipifarnib-like compounds by structure-based  pharmacophore, virtual screening and molecular docking against K-Ras  post-translation in colorectal cancer