Ras inhibition results in growth arrest and death of androgen-dependent and androgen-independent prostate cancer cells

Biochem Pharmacol. 2006 Aug 14;72(4):427-36. doi: 10.1016/j.bcp.2006.05.007. Epub 2006 May 13.

Abstract

Prostate cancer is one of the most frequently diagnosed cancers in human males. Progression of these tumors is facilitated by autocrine/paracrine growth factors which activate critical signaling cascades that promote prostate cancer cell growth, survival and migration. Among these, Ras pathways have a major role. Here we examined the effect of the Ras inhibitor S-trans, trans-farnesylthiosalicylic acid (FTS), on growth and viability of androgen-dependent and androgen-independent prostate cancer cells. FTS downregulated Ras, inhibited signaling to Akt and reduced the levels of cell-cycle regulatory proteins including cyclin D1, p-RB, E2F-1 and cdc42 in LNCaP and PC3 cells. Consequently the anchorage-dependent and anchorage-independent growth of LNCaP and PC3 cells were inhibited. FTS also induced apoptotic cell death which was inhibited by the broad-spectrum caspases inhibitor, Boc-asp-FMK. Our study demonstrated that androgen-dependent and androgen-independent prostate cancer cells require active Ras for growth and survival. Ras inhibition by FTS results in growth arrest and cell death. FTS may be qualified as a potential agent for the treatment of prostate cancer.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amino Acid Chloromethyl Ketones / pharmacology
  • Androgens / physiology*
  • Antineoplastic Agents / pharmacology
  • Apoptosis / drug effects*
  • Cell Cycle / drug effects
  • Cell Cycle Proteins / metabolism
  • Cell Line, Tumor
  • Cell Proliferation / drug effects*
  • Cell Survival / drug effects
  • Cyclin D1 / metabolism
  • Dose-Response Relationship, Drug
  • Down-Regulation / drug effects
  • E2F1 Transcription Factor / metabolism
  • Farnesol / analogs & derivatives*
  • Farnesol / pharmacology
  • Humans
  • Male
  • Myotonin-Protein Kinase
  • Prostatic Neoplasms / metabolism
  • Prostatic Neoplasms / pathology
  • Protein-Tyrosine Kinases / metabolism
  • Proto-Oncogene Proteins c-akt / metabolism
  • Salicylates / pharmacology*
  • Serine Proteinase Inhibitors / pharmacology
  • Signal Transduction / drug effects
  • ras Proteins / antagonists & inhibitors*
  • ras Proteins / metabolism
  • ras Proteins / physiology

Substances

  • Amino Acid Chloromethyl Ketones
  • Androgens
  • Antineoplastic Agents
  • Cell Cycle Proteins
  • E2F1 Transcription Factor
  • Salicylates
  • Serine Proteinase Inhibitors
  • butyloxycarbonyl-aspartyl-fluoromethyl ketone
  • farnesylthiosalicylic acid
  • Cyclin D1
  • Farnesol
  • CDC42BPB protein, human
  • Protein-Tyrosine Kinases
  • Myotonin-Protein Kinase
  • Proto-Oncogene Proteins c-akt
  • ras Proteins