Farnesyltransferase Inhibitors

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Farnesyl transferase inhibitors (FTIs) are a class of anti-tumor proximates that use the modification enzyme, farnesyl transferase (FTase), which is a cell-transformed molecular protein. The FTase-catalyzed farnesylation of Ras protein, the hydrophobic drone base can guide the farnesyl Ras protein target to localize to the cell membrane containing the hydrophobic group to mediate cell signal transduction. If the mutated Ras protein persists in the viable state, the cell signal is mediated, which can cause the cells to continue to grow and develop tumors. By inhibiting the activity of FTase and blocking the targeting of Ras protein, FTIs can effectively inhibit the proliferation of tumor cells.

Mechanism of action

Protein farnesylation refers to the transfer of farnesyl in the intermediate farnesyl pyrophosphate (FDP) of the cholesterol synthesis pathway to the C-terminus of the acceptor protein by the action of FTase. Among them, Ras protein farnesylation is one of the most important steps in its biological activity. The farnesyl transferase inhibitor can block the modification of the protein lipid by inhibiting farnesylation, and the Ras protein cannot be localized to the cell membrane. However, the Ras protein transduction signal has a certain positional requirement, that is, it must be stopped inside the cell, so its signal transduction function cannot be performed. As a result, the growth of tumors that depend on highly active Ras proteins is inhibited and their anticancer activity is exerted.

Application of Farnesyltransferase Inhibitors

FTIs are a class of anticancer drugs with potential application values. The use of farnesyl transferase inhibitors has become a new target for the molecular design of pharmaceuticals, which has attracted the attention of many well-known pharmaceutical research institutions and pharmaceutical companies. According to the structural analysis and catalytic mechanism studies, the research focuses on the following four types of compounds: (1) CAAX tetrapeptide (C: cysteine, X: any aliphatic amino acid, X: any amino acid) and its analogues; (2) farnesyl pyrophosphonate (FPP) mimetic; (3) double substrate mimic; (4) natural product. Among them, CAAX compounds have good specificity, strong ability to recognize enzymes, and easy to synthesize. They have carried out systematic research, and have synthesized hundreds of compounds and evaluated the biological activities. As a new drug that inhibits the activation of proto-oncogenes, farnesyltransferase inhibitors play a role in the inhibition of Ras mutant tumors.


  1. Klochkov, S. G, Neganova, M. E, Yarla, N. S. Parvathaneni, M, Sharma, B, & Tarasov, V. V, et al. (2017). Implications of farnesyltransferase and its inhibitors as a promising strategy for cancer therapy. Seminars in Cancer Biology.
  2. Shen, Y., Qiang, S., & Ma, S. (2015). The Recent Development of Farnesyltransferase Inhibitors as Anticancer and Antimalarial Agents. Mini reviews in medicinal chemistry, 15(10), 837-857.
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