Definition

An orally bioavailable inhibitor of farnesyl transferase, with potential antineoplastic activity. Upon oral administration, farnesyl transferase inhibitor (FTI) KO-2806 targets, binds to and inhibits the enzyme farnesyl transferase. By inhibiting the farnesylation of proteins, this agent prevents the activation of Ras oncogenes, inhibits Ras-dependent signaling and inhibits the proliferation of tumor cells in which Ras is overexpressed and/or mutated. Ras plays an important role in cell signaling, division and differentiation. Mutations of Ras may induce constitutive signal transduction leading to tumor cell growth, proliferation, invasion, and metastasis.