Farnesyl Derivatives of Rigid Carboxylic Acids-Inhibitors of ras-Dependent Cell Growth

Daniella Marciano, Gilad Ben-Baruch, Michal Marom, Yaakov Egozi, Roni Haklai, Yoel Kloog*

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review


Inhibitors of the enzyme that methylates ras proteins, the prenylated protein methyltransferase (PPMTase), are described. They are famesyl derivatives of rigid carboxylic acids that recognize the famesylcysteine recognition domain of the enzyme but do not serve as substrates. They also inhibit ras-dependent cell growth by a mechanism that is probably unrelated to inhibition of ras methylation, even though their potencies as PPMTase inhibitors and cell-growth inhibitors correlate well. The most potent inhibitor is S-trans,trans-farnesylthiosalicylic acid (FTS) (2). FTS (2) selectively inhibits the growth of human Ha-ras-transformed Rat1 cells in vitro (EC50 = 7.5 μM).

Original languageEnglish
Pages (from-to)1267-1272
Number of pages6
JournalJournal of Medicinal Chemistry
Issue number8
StatePublished - 1 Apr 1995


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