Document Detail

One-step (18)F-labeling of peptides for positron emission tomography imaging using the SiFA methodology.
MedLine Citation:
PMID:  23037309     Owner:  NLM     Status:  MEDLINE    
Here we present a procedure to label peptides with the positron-emitting radioisotope fluorine-18 ((18)F) using the silicon-fluoride acceptor (SiFA) labeling methodology. Positron emission tomography (PET) has gained high importance in noninvasive imaging of various diseases over the past decades, and thus new specific imaging probes for PET imaging, especially those labeled with (18)F, because of the advantageous properties of this nuclide, are highly sought after. N-terminally SiFA-modified peptides can be labeled with (18)F(-) in one step at room temperature (20-25 °C) or below without forming side products, thereby producing satisfactory radiochemical yields of 46 ± 1.5% (n = 10). The degree of chemoselectivity of the (18)F-introduction, which is based on simple isotopic exchange, allows for a facile cartridge-based purification fully devoid of HPLC implementation, thereby yielding peptides with specific activities between 44.4 and 62.9 GBq μmol(-1) (1,200-1,700 Ci mmol(-1)) within 25 min.
Carmen Wängler; Sabrina Niedermoser; Joshua Chin; Katy Orchowski; Esther Schirrmacher; Klaus Jurkschat; Liuba Iovkova-Berends; Alexey P Kostikov; Ralf Schirrmacher; Björn Wängler
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't     Date:  2012-10-04
Journal Detail:
Title:  Nature protocols     Volume:  7     ISSN:  1750-2799     ISO Abbreviation:  Nat Protoc     Publication Date:  2012 Nov 
Date Detail:
Created Date:  2012-10-05     Completed Date:  2013-03-19     Revised Date:  2013-03-21    
Medline Journal Info:
Nlm Unique ID:  101284307     Medline TA:  Nat Protoc     Country:  England    
Other Details:
Languages:  eng     Pagination:  1946-55     Citation Subset:  IM    
Biomedical Chemistry, Medical Research Center Mannheim, Medical Faculty Mannheim, Heidelberg University, Mannheim, Germany.
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MeSH Terms
Chromatography, High Pressure Liquid
Fluorine Radioisotopes*
Isotope Labeling / methods*
Organosilicon Compounds / analysis,  chemistry
Peptides / analysis*,  chemistry
Positron-Emission Tomography / methods*
Reg. No./Substance:
0/Fluorine Radioisotopes; 0/Organosilicon Compounds; 0/Peptides; 0/p-(di-tert-butyl((18)F)fluorosilyl)benzaldehyde

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine

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