Temsirolimus inhibits cell growth in combination with inhibitors of the B-cell receptor pathway

Leuk Lymphoma. 2015;56(12):3393-400. doi: 10.3109/10428194.2015.1023720. Epub 2015 Aug 3.

Abstract

Lately, mTOR inhibitors have gained clinical relevance in malignant lymphoma. Still, rapamycin derivatives may activate a pro-survival feedback loop through PI3K-Akt. In this current study, temsirolimus effectively reduced cell growth in GCB and ABC diffuse large cell B-cell lymphoma (GCB=30-66%, ABC=45-57%). Combination treatment with the PI3K-δ inhibitor idelalisib additively effected ABC and GCB lymphoma (GCB=16-38%, ABC=25-50%). Since Bruton's Tyrosine Kinase (BTK) plays a significant role for the survival of ABC lymphoma, this study also combined the BTK inhibitor ibrutinib with temsirolimus, which resulted in additive cell growth reduction (ibrutinib 50%, temsirolimus 44%, combination 25%) in ABC lymphoma. In contrast, bortezomib, which has been shown previously to be efficient in ABC lymphoma, revealed an antagonistic effect with temsirolimus in some GCB lymphoma (temsirolimus 53%, temsirolimus+bortezomib 63%). Western blot analysis identified the increase of phosphorylated pro-survival kinases Akt and PDK as a possible underlying mechanism of this interaction.

Keywords: DLBCL; PI3K; mTOR; temsirolimus.

MeSH terms

  • Adenine / analogs & derivatives
  • Antineoplastic Agents / pharmacology*
  • Bortezomib / pharmacology
  • Cell Cycle / drug effects
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Dose-Response Relationship, Drug
  • Drug Antagonism
  • Drug Synergism
  • Humans
  • Lymphoma, Large B-Cell, Diffuse / metabolism
  • Phosphatidylinositol 3-Kinases / metabolism
  • Phosphoinositide-3 Kinase Inhibitors
  • Phosphorylation
  • Piperidines
  • Protein Kinase Inhibitors / pharmacology*
  • Proto-Oncogene Proteins c-akt / metabolism
  • Purines / pharmacology
  • Pyrazoles / pharmacology
  • Pyrimidines / pharmacology
  • Quinazolinones / pharmacology
  • Receptors, Antigen, B-Cell / antagonists & inhibitors*
  • Receptors, Antigen, B-Cell / metabolism*
  • Signal Transduction / drug effects*
  • Sirolimus / analogs & derivatives*
  • Sirolimus / pharmacology

Substances

  • Antineoplastic Agents
  • Phosphoinositide-3 Kinase Inhibitors
  • Piperidines
  • Protein Kinase Inhibitors
  • Purines
  • Pyrazoles
  • Pyrimidines
  • Quinazolinones
  • Receptors, Antigen, B-Cell
  • ibrutinib
  • temsirolimus
  • Bortezomib
  • Proto-Oncogene Proteins c-akt
  • Adenine
  • Sirolimus
  • idelalisib