Inhibiting the palmitoylation/depalmitoylation cycle selectively reduces the growth of hematopoietic cells expressing oncogenic Nras

Blood. 2012 Jan 26;119(4):1032-5. doi: 10.1182/blood-2011-06-358960. Epub 2011 Dec 5.

Abstract

The palmitoylation/depalmitoylation cycle of posttranslational processing is a potential therapeutic target for selectively inhibiting the growth of hematologic cancers with somatic NRAS mutations. To investigate this question at the single-cell level, we constructed murine stem cell virus vectors and assayed the growth of myeloid progenitors. Whereas cells expressing oncogenic N-Ras(G12D) formed cytokine-independent colonies and were hypersensitive to GM-CSF, mutations within the N-Ras hypervariable region induced N-Ras mislocalization and attenuated aberrant progenitor growth. Exposing transduced hematopoietic cells and bone marrow from Nras and Kras mutant mice to the acyl protein thioesterase inhibitor palmostatin B had similar effects on protein localization and colony growth. Importantly, palmostatin B-mediated inhibition was selective for Nras mutant cells, and we mapped this activity to the hypervariable region. These data support the clinical development of depalmitoylation inhibitors as a novel class of rational therapeutics in hematologic malignancies with NRAS mutations.

Publication types

  • Research Support, American Recovery and Reinvestment Act
  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amino Acid Substitution
  • Animals
  • Antineoplastic Agents / pharmacology*
  • Cell Line, Transformed
  • Crosses, Genetic
  • Enzyme Inhibitors / pharmacology*
  • Hematologic Neoplasms / drug therapy
  • Hematopoietic Stem Cells / drug effects*
  • Hematopoietic Stem Cells / metabolism
  • Lipoylation / drug effects*
  • Mice
  • Mice, 129 Strain
  • Mice, Inbred C57BL
  • Mice, Mutant Strains
  • Molecular Targeted Therapy
  • Mutant Proteins / metabolism
  • Osmolar Concentration
  • Palmitoyl-CoA Hydrolase / antagonists & inhibitors*
  • Protein Processing, Post-Translational / drug effects*
  • Protein Transport
  • Proto-Oncogene Proteins p21(ras) / genetics
  • Proto-Oncogene Proteins p21(ras) / metabolism*

Substances

  • Antineoplastic Agents
  • Enzyme Inhibitors
  • Mutant Proteins
  • Palmitoyl-CoA Hydrolase
  • Proto-Oncogene Proteins p21(ras)