Strain-Promoted Copper-Free 'Click' Chemistry for 18F Radiolabeling of Bombesin

Autor: Anne K. Schoonen, Philippus Elsinga, Rudi Dierckx, Leila Mirfeizi, Lachlan S. Campbell-Verduyn, Bernard Feringa
Přispěvatelé: Stratingh Institute of Chemistry, Synthetic Organic Chemistry, Guided Treatment in Optimal Selected Cancer Patients (GUTS)
Rok vydání: 2011
Předmět:
Fluorine Radioisotopes
Peptide
Prostate cancer
chemistry.chemical_compound
Radioligand Assay
Radioligand
PEPTIDE
LIVING CELLS
GeneralLiterature_REFERENCE(e.g.
dictionaries
encyclopedias
glossaries)
radiopharmaceuticals
chemistry.chemical_classification
Molecular Structure
Chemistry
Bombesin
General Medicine
Amino acid
PROSTATE-CANCER
imaging agents
Biochemistry
Isotope Labeling
click chemistry
Click chemistry
ComputingMethodologies_DOCUMENTANDTEXTPROCESSING
hormones
hormone substitutes
and hormone antagonists
Protein Binding
Azides
Stereochemistry
Neuropeptide
3-DIPOLAR CYCLOADDITION
digestive system
complex mixtures
Binding
Competitive
Catalysis
Cell Line
Tumor
medicine
Humans
Copper-free click chemistry
isotopic labeling
RECEPTOR TARGETED RADIOPHARMACEUTICALS
ANALOGS
F-18
General Chemistry
medicine.disease
1
3-DIPOLAR CYCLOADDITION
Receptors
Bombesin
PET
Positron-Emission Tomography
peptides
LABELING METHOD
AZIDE-ALKYNE CYCLOADDITION
Copper
Zdroj: Angewandte Chemie-International Edition, 50(47), 11117-11120. WILEY-V C H VERLAG GMBH
ISSN: 0044-8249
1521-3773
DOI: 10.1002/ange.201105547
Popis: Bombesin is a 14 amino acid (Pyr-Gln-Arg-Leu-Gly-AsnGln-Trp-Ala-Val-Gly-His-Leu-Met-NH2) neuropeptide, which binds with high affinity to the gastrin-releasing peptide receptor (GRPR). Bombesin has received much attention in the field of nuclear imaging because the GRPR is massively overexpressed on a variety of tumor cells, including breast and prostate tumor cells, thus making bombesin a promising radioligand for the diagnosis and imaging of cancer. Much effort has been invested in the development of labeled bombesin analogues. Bombesin is often modified in the form of Lys[3]-bombesin, which allows for site-selective introduction of the radionuclide at the terminal amino
Databáze: OpenAIRE
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