| Autor: |
Elizabeth Cooper, Peter J. Choi, Kihwan Hwang, Kyung M. Nam, Chae‐Yong Kim, Tina Shaban, Patrick Schweder, Edward Mee, Jason Correia, Clinton Turner, Richard L. M. Faull, William A. Denny, Katsuya Noguchi, Mike Dragunow, Jiney Jose, Thomas I.‐H. Park |
| Rok vydání: |
2022 |
| Předmět: |
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| Zdroj: |
Chemical biologydrug designREFERENCES. |
| ISSN: |
1747-0285 |
| Popis: |
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 |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
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