Inhibitory effect of somatostatin Peptide analogues on DNA polymerase activity and human cancer cell proliferation

Anticancer Res. 2010 Dec;30(12):4841-9.


Background and objectives: It was previously reported that ten small peptides derived from TT-232, somatostatin structural analogue (compounds 1-10), synthesised by a solution-phase method, exhibited potent antitumour activity on human epithelial tumour (A431) cells.

Materials and methods: The present study investigated the inhibitory activity of these peptide compounds against DNA polymerase (pol) and human cancer cell growth.

Results: Among the compounds tested, compounds 1-5, which contain a t-butyloxycarbonyl (Boc) group, inhibited the activity of mammalian pols. Compounds 2 (Boc-Tyr-D-Trp-1-adamantylamide) and 3 (Boc-Tyr-D-Trp-2-adamantylamide) strongly suppressed the growth of a human colon carcinoma (HCT116) cell line and also arrested HCT116 cells in S phase, suggesting that these phenomena observed in cancer cells may be due to the selective inhibition of mammalian pols, especially DNA replicative pol α, by these compounds. Compound 2 induced apoptosis of the cells, although compound 3 did not.

Conclusion: Compounds 2 and 3 had an enhanced anticancer effect based on pol inhibition.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Cattle
  • Cell Cycle / drug effects
  • Cell Growth Processes / drug effects
  • Cell Survival / drug effects
  • DNA, Neoplasm / metabolism
  • DNA-Directed DNA Polymerase / metabolism
  • HCT116 Cells
  • Humans
  • Models, Molecular
  • Nucleic Acid Synthesis Inhibitors*
  • Peptides / pharmacology*
  • Rats
  • Somatostatin / analogs & derivatives*
  • Somatostatin / pharmacology


  • DNA, Neoplasm
  • Nucleic Acid Synthesis Inhibitors
  • Peptides
  • Somatostatin
  • DNA-Directed DNA Polymerase