MG132 inhibits proliferation and induces apoptosis of acute lymphoblastic leukemia via Akt/FOXO3a/Bim pathway

Hum Exp Toxicol. 2024 Jan-Dec:43:9603271241303030. doi: 10.1177/09603271241303030.

Abstract

Background: Acute lymphoblastic leukemia (ALL) is one of the most common pediatric cancers, characterized by the malignant proliferation of leukemic cells. Despite advancements in treatment, the prognosis for refractory and relapsed ALL remains poor, underscoring the need for novel therapeutic targets and approaches.

Methods: To investigate the anti-leukemic properties of MG132, MTS assays were employed to assess cell viability, and flow cytometry was used to evaluate apoptosis. Mechanistic studies, including qRT-PCR, Western blotting, and lentivirus-mediated FOXO3a knockdown, were conducted to explore MG132's effects on the Akt/FOXO3a/Bim signaling pathway. A xenograft mouse model was utilized to validate the in vivo efficacy of MG132 in suppressing tumor growth.

Results: MG132 inhibited cell proliferation and induced apoptosis in both ALL cell lines and primary cells in a concentration-dependent manner. Mechanistic studies revealed that MG132 promoted FOXO3a nuclear localization by suppressing Akt phosphorylation and preventing FOXO3a degradation, leading to increased Bim expression. Furthermore, FOXO3a knockdown significantly reduced MG132's anti-proliferative effects. In vivo, MG132 markedly inhibited tumor growth in the xenograft model.

Conclusion: These findings suggest that MG132 exerts potent anti-leukemic effects through modulation of the Akt/FOXO3a/Bim axis, offering a promising therapeutic avenue for treating ALL.

Keywords: Akt; Bim; FOXO3a; MG132; acute lymphoblastic leukemia.

MeSH terms

  • Animals
  • Antineoplastic Agents / pharmacology
  • Antineoplastic Agents / therapeutic use
  • Apoptosis* / drug effects
  • Bcl-2-Like Protein 11* / genetics
  • Bcl-2-Like Protein 11* / metabolism
  • Cell Line, Tumor
  • Cell Proliferation* / drug effects
  • Forkhead Box Protein O3* / genetics
  • Forkhead Box Protein O3* / metabolism
  • Humans
  • Leupeptins / pharmacology
  • Leupeptins / therapeutic use
  • Mice
  • Precursor Cell Lymphoblastic Leukemia-Lymphoma* / drug therapy
  • Precursor Cell Lymphoblastic Leukemia-Lymphoma* / metabolism
  • Proto-Oncogene Proteins c-akt* / metabolism
  • Signal Transduction / drug effects
  • Xenograft Model Antitumor Assays

Substances

  • Forkhead Box Protein O3
  • Bcl-2-Like Protein 11
  • Proto-Oncogene Proteins c-akt
  • FOXO3 protein, human
  • benzyloxycarbonylleucyl-leucyl-leucine aldehyde
  • Leupeptins
  • Antineoplastic Agents