多肽的固相直接 18F 放射氟化。

IF 2.5 4区 医学 Q3 CHEMISTRY, MEDICINAL Bioorganic & Medicinal Chemistry Letters Pub Date : 2025-01-30 DOI:10.1016/j.bmcl.2025.130118
Eduardo F.A. Fernandes , Line B.S. Knudsen , Andreas Kjaer , Kristian Strømgaard , Matthias M. Herth
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Solid-phase supported direct 18F-radiofluorination of peptides
The absence of universal and expedient labeling procedures hampers the widespread application of peptides as molecular tracers for positron emission tomography (PET). In this work, we have developed a proof-of-concept direct radiofluorination procedure for peptides using conventional solid-phase peptide synthesis. The method is compatible with all standard amino acids and enables the generation of a range of peptide-based radiopharmaceuticals archieving radiochemical yields of up to 30 % and radiochemical purities above 95 %.
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来源期刊
CiteScore
5.70
自引率
3.70%
发文量
463
审稿时长
27 days
期刊介绍: Bioorganic & Medicinal Chemistry Letters presents preliminary experimental or theoretical research results of outstanding significance and timeliness on all aspects of science at the interface of chemistry and biology and on major advances in drug design and development. The journal publishes articles in the form of communications reporting experimental or theoretical results of special interest, and strives to provide maximum dissemination to a large, international audience.
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Editorial Board Contents continued Graphical abstract TOC Graphical abstract TOC Oxime functionalized Chalcones: Unveiling a new class of Chalcones with potent Antiplasmodial activity against blood-stages of plasmodium falciparum in culture.
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