2532-07-2Relevant articles and documents
18F-Fluorination of Unactivated C-H Bonds in Branched Aliphatic Amino Acids: Direct Synthesis of Oncological Positron Emission Tomography Imaging Agents
Nodwell, Matthew B.,Yang, Hua,?olovi?, Milena,Yuan, Zheliang,Merkens, Helen,Martin, Rainer E.,Bénard, Fran?ois,Schaffer, Paul,Britton, Robert
, p. 3595 - 3598 (2017)
A mild and selective photocatalytic C-H 18F-fluorination reaction has been developed that provides direct access to 18F-fluorinated amino acids. The biodistribution and uptake of three 18F-labeled leucine analogues via LAT1 mediated transport in several cancer cell lines is reported. Positron emission tomography imaging of mice bearing PC3 (prostate) or U87 (glioma) xenografts using 5-[18F]-fluorohomoleucine showed high tumor uptake and excellent tumor visualization, highlighting the utility of this strategy for rapid tracer discovery for oncology.
Site-Selective, Late-Stage C?H 18F-Fluorination on Unprotected Peptides for Positron Emission Tomography Imaging
Yuan, Zheliang,Nodwell, Matthew B.,Yang, Hua,Malik, Noeen,Merkens, Helen,Bénard, Fran?ois,Martin, Rainer E.,Schaffer, Paul,Britton, Robert
supporting information, p. 12733 - 12736 (2018/09/12)
Peptides are often ideal ligands for diagnostic molecular imaging due to their ease of synthesis and tuneable targeting properties. However, labelling unmodified peptides with 18F for positron emission tomography (PET) imaging presents a number of challenges. Here we show the combination of photoactivated sodium decatungstate and [18F]-N-fluorobenzenesulfonimide effects site-selective 18F-fluorination at the branched position in leucine residues in unprotected and unaltered peptides. This streamlined process provides a means to directly convert native peptides into PET imaging agents under mild aqueous conditions, enabling rapid discovery and development of peptide-based molecular imaging tools.