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Elucidating the cellular uptake mechanisms of heptamethine cyanine dye analogues for their use as an anticancer drug-carrier molecule for the treatment of glioblastoma
- Source :
- Chemical biologydrug designREFERENCES.
- Publication Year :
- 2022
-
Abstract
- The development of chemotherapies for glioblastoma is hindered by their limited bioavailability and toxicity on normal brain function. To overcome these limitations, we investigated the structure-dependent activity of heptamethine cyanine dyes (HMCD), a group of tumour-specific and BBB permeable near-infrared fluorescent dyes, in both commercial (U87MG) and patient-derived GBM cell lines. HMCD analogues with strongly ionisable sulphonic acid groups were not taken up by patient-derived GBM cells, but were taken up by the U87MG cell line. HMCD uptake relies on a combination of transporter uptake through organic anion-transporting polypeptides (OATPs) and endocytosis into GBM cells. The uptake of HMCDs was not affected by p-glycoprotein efflux in GBM cells. Finally, we demonstrate structure-dependent cytotoxic activity at high concentrations (EC
- Subjects :
- Pharmacology
Drug Discovery
Organic Chemistry
Molecular Medicine
Biochemistry
Subjects
Details
- ISSN :
- 17470285
- Database :
- OpenAIRE
- Journal :
- Chemical biologydrug designREFERENCES
- Accession number :
- edsair.doi.dedup.....a7b9812c550b917d6fe592d96f78ba8f