Runx2 silencing sensitized human renal cell carcinoma cells to ABT-737 apoptosis

Arch Biochem Biophys. 2024 Nov:761:110173. doi: 10.1016/j.abb.2024.110173. Epub 2024 Oct 5.

Abstract

The prognostic value of Runt-related transcription factor 2 (Runx2) and its involvement in cell growth and motility have been reported in patients diagnosed with renal cell carcinoma (RCC). Since Runx2 may have the potential to be a target for the purpose of antitumor intervention, there is an urgent need to gain insight into its oncogenic properties. Using human 786-O, Caki-1 and ACHN RCC cells as models, the silencing of cellular Runx2 expression brought about a reduction in cyclin D1 and β-catenin expression, cell growth and migration without any significant cell death. Runx2-silenced cells turned into apoptosis vulnerable in the presence of ABT-737, a BH3 mimetic Bcl-2 inhibitor. Data from biochemical and molecular studies have revealed a positive correlation between Runx2 expression and Akt phosphorylation, Mcl-1 expression, and fibronectin expression. Results of genetic silencing studies have indicated the potential involvement of Mcl-1 and fibronectin in the decision of RCC cell ABT-737 resistance and sensitivity. The regulatory roles of the PI3K/Akt axis in the expression of Mcl-1 and fibronectin were suggested by means of the results taken from experiments involving pharmacological study of the PI3K/Akt. Since overexpression and prognostic roles of Runx2, activated Akt, Mcl-1, fibronectin, cyclin D1, and β-catenin have been revealed in RCC, it is important to explore the precise mechanisms underlying Runx2 oncogenic effects. Although the linking details between Runx2 and PI3K/Akt have yet to be identified, our findings suggest that Mcl-1 and fibronectin are downstream effectors of Runx2 via a regulatory axis of the PI3K/Akt and their promotion of cell growth, migration, and ABT-737 resistance in RCC cells.

Keywords: ABT-737; Akt; Renal cell carcinoma; Runx2.

MeSH terms

  • Antineoplastic Agents / pharmacology
  • Apoptosis* / drug effects
  • Biphenyl Compounds* / pharmacology
  • Carcinoma, Renal Cell* / drug therapy
  • Carcinoma, Renal Cell* / genetics
  • Carcinoma, Renal Cell* / metabolism
  • Carcinoma, Renal Cell* / pathology
  • Cell Line, Tumor
  • Cell Movement / drug effects
  • Cell Proliferation / drug effects
  • Core Binding Factor Alpha 1 Subunit* / genetics
  • Core Binding Factor Alpha 1 Subunit* / metabolism
  • Cyclin D1 / genetics
  • Cyclin D1 / metabolism
  • Gene Silencing*
  • Humans
  • Kidney Neoplasms* / drug therapy
  • Kidney Neoplasms* / genetics
  • Kidney Neoplasms* / metabolism
  • Kidney Neoplasms* / pathology
  • Myeloid Cell Leukemia Sequence 1 Protein / genetics
  • Myeloid Cell Leukemia Sequence 1 Protein / metabolism
  • Nitrophenols* / pharmacology
  • Phosphatidylinositol 3-Kinases / metabolism
  • Piperazines* / pharmacology
  • Proto-Oncogene Proteins c-akt / metabolism
  • Sulfonamides* / pharmacology
  • beta Catenin / metabolism

Substances

  • Nitrophenols
  • ABT-737
  • Biphenyl Compounds
  • Sulfonamides
  • Core Binding Factor Alpha 1 Subunit
  • Piperazines
  • RUNX2 protein, human
  • Proto-Oncogene Proteins c-akt
  • Cyclin D1
  • Myeloid Cell Leukemia Sequence 1 Protein
  • beta Catenin
  • Phosphatidylinositol 3-Kinases
  • MCL1 protein, human
  • Antineoplastic Agents