Inhibition of growth and invasive activity of human pancreatic cancer cells by a farnesyltransferase inhibitor, manumycin

Pancreas. 1997 Nov;15(4):379-83. doi: 10.1097/00006676-199711000-00008.

Abstract

The effects of manumycin, a competitive farnesyltransferase (FTase) inhibitor, on pancreatic cancer cell lines with or without K-ras mutation were studied. Manumycin inhibited the growth of human pancreatic cancer cells (SUIT-2, MIA PaCa-2, AsPC-1, BxPC-3) in a dose-dependent manner. The 50% inhibitory concentration (IC50) in cell lines with a mutant K-ras gene (SUIT-2, MIA PaCa-2, AsPC-1) was lower than that in BxPC-3 with a wild-type ras. Both mitogen-activated protein kinase activity after growth stimuli and the ability for chemotactic invasion were markedly more inhibited by manumycin in SUIT-2 than in BxPC-3. These results suggest that mutated Ras is more sensitive to manumycin than the wild type. Furthermore, tumor growth and liver metastasis in nude mice inoculated with manumycin-treated SUIT-2 cells were inhibited dose dependently. Inhibition of Ras activity might be a new anticancer strategy in pancreatic cancer in which Ras plays a role.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alkyl and Aryl Transferases / antagonists & inhibitors*
  • Animals
  • Antineoplastic Agents / pharmacology*
  • DNA, Neoplasm / biosynthesis
  • Enzyme Inhibitors / pharmacology*
  • Farnesyltranstransferase
  • Genes, ras / genetics
  • Humans
  • Liver Neoplasms / secondary
  • Mice
  • Mice, Nude
  • Neoplasm Invasiveness
  • Pancreatic Neoplasms / genetics
  • Pancreatic Neoplasms / metabolism
  • Pancreatic Neoplasms / pathology*
  • Point Mutation
  • Polyenes / pharmacology*
  • Polyunsaturated Alkamides
  • Protein Kinases / metabolism
  • Tumor Cells, Cultured

Substances

  • Antineoplastic Agents
  • DNA, Neoplasm
  • Enzyme Inhibitors
  • Polyenes
  • Polyunsaturated Alkamides
  • Alkyl and Aryl Transferases
  • Farnesyltranstransferase
  • Protein Kinases
  • manumycin