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September 8, 2026ChemMedChem

Substituent Effects of Heptamethine Cyanine Dyes on Drug Uptake in Patient‐Derived Glioma Cells

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Authors

CDCarina J. DumoPCPeter J. ChoiYLYuge Liu

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Overview

In vitro study demonstrates enhanced drug uptake and potency using dye-conjugated crizotinib in patient-derived glioblastoma cells, highlighting a promising delivery strategy across brain barriers.

Key Points

  • To determine how chemical substituents on blood–brain barrier-crossing heptamethine cyanine dyes affect cellular uptake and anticancer potency when conjugated to crizotinib.
  • Synthesized conjugates linking the targeted kinase inhibitor crizotinib to heptamethine cyanine dyes modified with distinct functional groups.
  • Evaluated in vitro cellular uptake and antiproliferative activity across four patient-derived glioblastoma cell lines.
  • Heptamethine cyanine dye functionalization enhanced intracellular delivery of crizotinib across all evaluated patient-derived cell models.
  • Increased intracellular conjugate accumulation directly improved cytotoxic potency relative to parent compounds.

Cite This Study

Dumo et al. (2026) studied this question.

synapsesocial.com/papers/6a9fd7d558e84d0ff5b46dbehttps://doi.org/10.1002/cmdc.70486
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  1. 1Modulation of blood-tumor barrier transcriptional programs improves intra-tumoral drug delivery and potentiates chemotherapy in GBM2024
  2. 2HGG-05. GLUCOSE CONJUGATION FOR THE SPECIFIC TARGETING AND TREATMENT OF GLIOBLASTOMA2024
  3. 3DDEL-26. Modulation of the Blood-Tumor Barrier Using Small-Molecule Inhibitors: Enhancing Chemotherapeutic Penetration in Glioblastoma Therapy2025
  4. 4EXTH-79. Functional Precision Medicine In Glioblastoma: Advancing Drug Screening With Patient-Derived 3D Cultures And Advanced Imaging Analyses2025
  5. 5Abstract 7178: Targeted modulation of the blood-tumor barrier enhances drug delivery and survival in glioblastoma models2026