Abstract
We hypothesized that conjugation of the near-infrared dye MHI-148 with the anti-leukemia drug dasatinib might produce a potential theranostic for glioblastoma. In fact, the conjugate was found to bind the kinases Src and Lyn, and to inhibit the viability of a glioblastoma cell line with significantly greater potency than dasatinib alone, MHI-148 alone, or a mixture of dasatinib and MHI-148 at the same concentration. It was also used to successfully image a subcutaneous glioblastoma tumor in vivo.
Keywords:
cancer; cyanine; glioblastoma; imaging agents; tumor targeting.
© 2019 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim.
Publication types
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Research Support, Non-U.S. Gov't
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Research Support, U.S. Gov't, Non-P.H.S.
MeSH terms
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Animals
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Antineoplastic Agents / chemical synthesis
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Antineoplastic Agents / therapeutic use*
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Carbocyanines / chemistry
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Carbocyanines / therapeutic use*
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Cell Line, Tumor
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Dasatinib / chemical synthesis
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Dasatinib / therapeutic use*
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Drug Design
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Female
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Fluorescent Dyes / chemical synthesis
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Fluorescent Dyes / therapeutic use*
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Glioblastoma / drug therapy*
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Humans
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Indoles / chemical synthesis
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Indoles / chemistry
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Indoles / therapeutic use*
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Mice, Nude
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Protein Kinase Inhibitors / chemical synthesis
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Protein Kinase Inhibitors / therapeutic use*
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Theranostic Nanomedicine / methods
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Xenograft Model Antitumor Assays
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src-Family Kinases / antagonists & inhibitors
Substances
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Antineoplastic Agents
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Carbocyanines
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Fluorescent Dyes
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Indoles
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MHI-148
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Protein Kinase Inhibitors
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lyn protein-tyrosine kinase
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src-Family Kinases
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Dasatinib