Highly Fluorinated Peptide Probes with Enhanced In Vivo Stability for $^{19}$F‐MRI

Autor: Beibei Meng, Stephan L. Grage, Oleg Babii, Masanari Takamiya, Neil MacKinnon, Tim Schober, Illia Hutskalov, Omar Nassar, Sergii Afonin, Serhii Koniev, Igor V. Komarov, Jan G. Korvink, Uwe Strähle, Anne S. Ulrich
Jazyk: angličtina
Rok vydání: 2022
Předmět:
Zdroj: Small, 18 (41), Art.Nr. 2107308
ISSN: 1613-6810
1613-6829
DOI: 10.5445/ir/1000150903
Popis: A labeling strategy for in vivo $^{19}$F-MRI (magnetic resonance imaging) based on highly fluorinated, short hydrophilic peptide probes, is developed. As dual-purpose probes, they are functionalized further by a fluorophore and an alkyne moiety for bioconjugation. High fluorination is achieved by three perfluoro-tert-butyl groups, introduced into asparagine analogues by chemically stable amide bond linkages. d-amino acids and β-alanine in the sequences endow the peptide probes with low cytotoxicity and high serum stability. This design also yielded unstructured peptides, rendering all 27 $^{19}$F substitutions chemically equivalent, giving rise to a single $^{19}$F-NMR resonance with
Databáze: OpenAIRE
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