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Doxorubicin prodrug-based nanomedicines for the treatment of cancer

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Summary: Mitochondria has been identified as a target for tumor therapy. This study developed a mitochondria-targeting anticancer agent, MT-1, which specifically accumulates in mitochondria and binds to GR. MT-1 damages the morphology and function of mitochondria, inhibits mitochondrial respiration and glycolysis, and binds to a new site of GR to inhibit its activity. This provides a potential novel strategy for tumor therapy by targeting novel sites of GR in mitochondria.

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Summary: Immune checkpoint inhibitors (ICIs) are a promising class of immunotherapy drugs that enhance the immune response in cancer treatment. In this study, a conjugate of doxorubicin (DOX) and isoniazid (INH), a MAOA inhibitor, was synthesized and shown to enhance CD8(+) T cell activity and exhibit synergistic anti-tumor effects. Additionally, DOX-INH inhibited the growth and metastasis of breast cancer by blocking specific signaling pathways. This small molecule conjugate has great potential in cancer therapy.

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Structure-Activity Relationship of pH-Sensitive Doxorubicin-Fatty Acid Prodrug Albumin Nanoparticles

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Summary: Albumin has been used as a versatile drug carrier, and researchers have synthesized acid-labile DOX prodrugs using different fatty acids as albumin-binding motifs. These prodrugs assembled albumin nanoparticles with ultrahigh drug loading, and their colloidal stability depended on the saturation of fatty acids, impacting their in vivo pharmacokinetics, tumor accumulation, and antitumor efficacy. The hydrazone bond-bridged prodrugs could release DOX in the acidic tumor environment, resulting in improved antitumor efficacy and safety.

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Nanoalbumin-prodrug conjugates prepared via a thiolation-and-conjugation method improve cancer chemotherapy and immune checkpoint blockade therapy by promoting CD8+ T-cell infiltration

Long Chen et al.

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Ning Liu et al.

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BIOORGANIC CHEMISTRY (2023)

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Ritesh Pal et al.

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Xianghui Zhu et al.

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Jianping Liu et al.

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