Radio-labeled probes, synthesis

Lee CC, Sui GD, Elizarov A, Shu CYJ, Shin YS, Dooley AN, Huang J, Dari-don A, Wyatt P, Stout D, Kolb HC, Witte ON, Satyamurthy N, Heath JR, Phelps ME, Quake SR, Tseng HR (2005) Multistep Synthesis of a Radio-labeled Imaging Probe Using Integrated Microfluidics. Science 310 1793— 1796... 

While the majority of the chemistry strategies and synthesis design is equivalent to standard analogue producing approaches, a unique feature can be taken into account based on the relative photosensitivity of the probes. The introduction of the radio or other types of labels can also modify the reaction sequences. 

To make these substrates suitable for biological assays, the introduction of functional groups that can be traced with the proper analytical techniques is essential. The use of radio-, fluorescent-, and biotin-labeled lipidated peptides has been reported. The synthesis of fluorescent substrates is chemically straightforward and allows for production of larger quantities than the enzymatic synthesis used for radiolabeled peptides and is thus preferred over the use of radioactive compounds. [1 21] Common fluorescent probes can be introduced by conjugation to a free functional group present in the peptide. The fluorescent moiety is... 

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