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Chloroethylnitrosourea analogue HJ03 overcomes temozolomide resistance of glioblastoma in mice through induction of ferroptosis and apoptosis - PubMed

4 hours ago
  • #chemoresistance
  • #glioblastoma
  • #ferroptosis
  • HJ03, a chloroethylnitrosourea analogue, overcomes temozolomide (TMZ) resistance in glioblastoma (GBM) by inducing ferroptosis and apoptosis.
  • HJ03 is more potent than TMZ in inhibiting GBM cell lines, including those with MGMT overexpression or MMR dysfunction.
  • HJ03 induces DNA damage and ferroptosis, leading to cell cycle arrest (G2/M phase) and apoptosis in GBM cells.
  • HJ03 upregulates p53 and ATF3 while downregulating SLC7A11, causing ROS and Fe2+ accumulation and increased MDA levels.
  • HJ03 crosses the blood-brain barrier more efficiently than TMZ and shows lower bone marrow toxicity.
  • In mice with orthotopic GBM tumors, HJ03 significantly prolonged lifespan and synergized with radiotherapy and anti-PD-1 therapy.
  • HJ03 is a promising candidate for treating TMZ-resistant GBM.