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Strain‐Promoted Copper‐Free “Click” Chemistry for 18 F Radiolabeling of Bombesin
Author(s) -
CampbellVerduyn Lachlan S.,
Mirfeizi Leila,
Schoonen Anne K.,
Dierckx Rudi A.,
Elsinga Philip H.,
Feringa Ben L.
Publication year - 2011
Publication title -
angewandte chemie international edition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 5.831
H-Index - 550
eISSN - 1521-3773
pISSN - 1433-7851
DOI - 10.1002/anie.201105547
Subject(s) - click chemistry , bombesin , azide , chemistry , copper , peptide , in vitro , strain (injury) , combinatorial chemistry , alkyne , receptor , biophysics , radiochemistry , biochemistry , organic chemistry , biology , catalysis , medicine , neuropeptide
Click for PET : The GRP‐receptor‐specific peptide bombesin, which is often used for nuclear imaging of tumors, can be labeled with 18 F in a mild and rapid manner by using a copper‐free azide–alkyne “click” reaction. A range of azides can be used to provide peptides with different hydrophobicities. The resulting 18 F radiopharmaceutical tracers (see scheme) maintain their high affinity for the targeted receptor in vitro in human prostate cancer cells.