Syntheses of fluorescent imidazoquinoline conjugates as probes of Toll-like receptor 7
| Autor: | Sunil A. David, Hemamali J. Warshakoon, Rehman Ukani, Nikunj M. Shukla, David S. Moore, Cole A. Mutz |
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| Rok vydání: | 2010 |
| Předmět: |
Clinical Biochemistry
Pharmaceutical Science Biochemistry Article Flow cytometry Cell Line chemistry.chemical_compound Mice Structure-Activity Relationship Drug Discovery medicine Fluorescence microscope Animals Humans Receptor Molecular Biology Fluorescent Dyes medicine.diagnostic_test Organic Chemistry TLR7 Ligand (biochemistry) Flow Cytometry Immunological Synapses In vitro Lymphocyte Subsets Imidazoquinoline chemistry Microscopy Fluorescence Toll-Like Receptor 7 Quinolines Molecular Medicine |
| Zdroj: | Bioorganicmedicinal chemistry letters. 20(22) |
| ISSN: | 1464-3405 |
| Popis: | Toll-like receptor (TLR)-7 agonists show prominent immunostimulatory activities. The synthesis of a TLR7-active N(1)-(4-aminomethyl)benzyl substituted imidazoquinoline 5d served as a convenient precursor for the covalent attachment of fluorophores without significant loss of activity. Fluorescence microscopy experiments show that the fluorescent analogues are internalized and distributed in the endosomal compartment. Flow cytometry experiments using whole human blood show differential partitioning into B, T, and natural killer (NK) lymphocytic subsets, which correlate with the degree of activation in these subsets. These fluorescently-labeled imidazoquinolines will likely be useful in examining the trafficking of TLR7 in immunological synapses. |
| Databáze: | OpenAIRE |
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