NVP-2, in combination with Orlistat, represents a promising therapeutic strategy for acute myeloid leukemia

Cancer Biol Ther. 2025 Dec;26(1):2450859. doi: 10.1080/15384047.2025.2450859. Epub 2025 Jan 12.

Abstract

Cell cycle dysregulation and the corresponding metabolic reprogramming play significant roles in tumor development and progression. CDK9, a kinase that regulates gene transcription and cell cycle, also induces oncogene transcription and abnormal cell cycle in AML cells. The function of CDK9 for gene regulation in AML cells requires further exploration. In this study, we knocked down the CDK9 to investigate its effects on the growth and survival of AML cells. Through RNA-seq analysis, we identified that in U937 cells CDK9 regulates numerous genes involved in proliferation and apoptosis, including mTOR, SREBF1, and Bcl-2. Furthermore, our results demonstrated that both CDK9 and FASN are crucial for the proliferation and survival of Kasumi-1 and U937 cells. Mechanistically, MCL1, c-Myc, and Akt/mTOR/SREBF1 may be critical factors and pathways in the combined therapy of NVP-2 and Orlistat. In summary, our study revealed that CDK9 and FASN are vital for maintaining AML cell survival and proliferation. Treatment with NVP-2 and Orlistat may be a promising clinical candidate for patients with AML.

Keywords: Acute myeloid leukemia; CDK9; FASN; SREBF1; apoptosis; c-Myc; cell proliferation; molecular targeted therapy.

MeSH terms

  • Antineoplastic Combined Chemotherapy Protocols / pharmacology
  • Antineoplastic Combined Chemotherapy Protocols / therapeutic use
  • Apoptosis / drug effects
  • Cell Line, Tumor
  • Cell Proliferation* / drug effects
  • Cyclin-Dependent Kinase 9* / antagonists & inhibitors
  • Cyclin-Dependent Kinase 9* / genetics
  • Cyclin-Dependent Kinase 9* / metabolism
  • Fatty Acid Synthase, Type I / antagonists & inhibitors
  • Fatty Acid Synthase, Type I / genetics
  • Fatty Acid Synthase, Type I / metabolism
  • Humans
  • Leukemia, Myeloid, Acute* / drug therapy
  • Leukemia, Myeloid, Acute* / genetics
  • Leukemia, Myeloid, Acute* / metabolism
  • Leukemia, Myeloid, Acute* / pathology
  • Myeloid Cell Leukemia Sequence 1 Protein / genetics
  • Myeloid Cell Leukemia Sequence 1 Protein / metabolism
  • Orlistat* / pharmacology
  • Orlistat* / therapeutic use
  • TOR Serine-Threonine Kinases / metabolism

Substances

  • Orlistat
  • Cyclin-Dependent Kinase 9
  • CDK9 protein, human
  • Fatty Acid Synthase, Type I
  • FASN protein, human
  • Myeloid Cell Leukemia Sequence 1 Protein
  • TOR Serine-Threonine Kinases
  • MCL1 protein, human