Farnesyl Thiosalicylic Acid

Farnesyl thiosalicylic acid (FTS) is an inhibitor of Ras-mediated signaling that functions by dislodging Ras from the cell membrane thereby rendering it susceptible to proteolytic degradation.¹ FTS inhibits the growth of human Ha-ras-transformed Rat1 fibroblasts with an IC₅₀ value of 7.5 µM.² It does not inhibit Ras farnesylation in vitro and although FTS does inhibit prenylated protein methyltransferase (PPMTase) in cell-free systems with a K_i value of 2.6 µM, it is relatively ineffective at inhibiting methylation in whole cells.³ Treatment of chow-fed ApoE-deficient mice with 5 mg/kg FTS three times per week for six weeks reduces early atherosclerotic lesion development by 52% compared to controls.⁴

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1. Haklai, R., Weisz, M.G., Elad, G., et al. Dislodgment and accelerated degradation of ras. Biochemistry 37(5), 1306-1314 (1998).

2. Marciano, D., Ben-Baruch, G., Marom, M., et al. Farnesyl derivatives of rigid carboxylic acids-inhibitors of ras-dependent cell growth. J. Med. Chem. 38(8), 1267-1272 (1995).

3. Marom, M., Haklai, R., Ben-Baruch, G., et al. Selective inhibition of ras-dependent cell growth by farnesylthiosalicylic acid. The Journal of Biological Chemisty 270(38), 22263-22270 (1995).

4. George, J., Afek, A., Keren, P., et al. Functional inhibition of ras by S-trans, trans-farnesyl thiosalicylic acid attenuates atherosclerosis in apolipoprotein E knockout mice. Circulation 105(20), 2416-2422 (2002).

Rodrigues, A.A., Clemente, T.M., dos Santos, M.A., et al. A recombinant protein based on Trypanosoma cruzi P21 enhances phagocytosis. PLos One 7(12), e51384 (2012).