Universal polyethylene glycol linkers for attaching receptor ligands to quantum dots
| Autor: | Elaine Sanders-Bush, Ian D. Tomlinson, Sandra J. Rosenthal, David M. Hercules, Anthony P. Gies, Paul J. Gresch, Joel Dillard, Rebecca L. Orndorff |
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| Rok vydání: | 2006 |
| Předmět: |
medicine.drug_class
Stereochemistry Clinical Biochemistry Pharmaceutical Science Receptors Cell Surface Carboxamide Polyethylene glycol Conjugated system Ligands Biochemistry Chemical synthesis Polyethylene Glycols chemistry.chemical_compound Drug Discovery medicine Molecular Biology Cell Membrane Organic Chemistry Combinatorial chemistry Small molecule Membrane Nanocrystal chemistry Quantum dot Spectrometry Mass Matrix-Assisted Laser Desorption-Ionization Quantum Theory Molecular Medicine |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 16:6262-6266 |
| ISSN: | 0960-894X |
| Popis: | Biologically active small molecule derivatives that can be conjugated to quantum dots have the promise of revolutionizing fluorescent imaging in biology. In order to achieve this several technical hurdles have to be surmounted, one of which is non-specific adsorption of quantum dots to cell membranes. Pegylating quantum dots has been shown to eliminate non-specific binding. Consequently it is necessary to develop a universal synthetic methodology to attach small molecule ligands to polyethylene glycol. These pegylated small molecules may then be conjugated to the surfaces of quantum dots. Ideally this universal strategy should be adaptable and be applicable to PEG chains of varying lengths. This paper describes the development of one such methodology and the synthesis of a pegylated derivative of the known 5HT 2 agonist 1-(2-aminopropyl)-2,5-dimethoxy benzene. This compound was tested and found to be an agonist for the 5HT 2A and 5HT 2C receptor having EC 50 values of 250 and 50 nM, respectively. |
| Databáze: | OpenAIRE |
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