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α-hydroxy Farnesyl Phosphonic Acid is a non-hydrolyzable analog of farnesyl pyrophosphate which acts as a competitive inhibitor of Farnesyl Transferase (FPTase). α-hydroxy Farnesyl Phosphonic acid inhibits the processing of Ras in Ha-ras-transformed NIH3T3 cells at concentrations greater than 1 μM.
1 Pompliano, D.L., Rands, E., Schaber, M.D., et al. Steady-state kinetic mechanism of ras farnesyl: Protein transferase. Biochemistry 31 3800-3807 (1992). 2 Hohl, R.J., Lewis, K.A., Cermak, D.M., et al. Stereochemistry-dependent inhibition of Ras farnesylation by farnesylphosphonic acids. Lipids 33 39-46 (1998). 3 Gibbs, J.B., Pompliano, D.L., Mosser, S.D., et al. Selective inhibition of farnesyl-protein transferase blocks ras processing in vivo. J Biol Chem 268 7617-7620 (1993).
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