TY - JOUR
T1 - Site-selective three-component reaction for dual-functionalization of peptides
AU - Munch, Henrik Kofoed
AU - Rasmussen, Jakob Ewald
AU - Popa, Gina
AU - Christensen, Jørn Bolstad
AU - Jensen, K.J.
PY - 2013/2/7
Y1 - 2013/2/7
N2 - A site-selective dual-functionalization of peptides is presented, involving readily available maleimides as well as N-hydroxylamines. The modification proceeds through a three component 1,3-dipolar cycloaddition, forming a stable product. This was exemplified by the one-pot attachment of two molecular imaging moieties to a tumor binding cyclic peptide, and was extended to the conjugation of a DOTA chelator to a 12 kDa protein.
AB - A site-selective dual-functionalization of peptides is presented, involving readily available maleimides as well as N-hydroxylamines. The modification proceeds through a three component 1,3-dipolar cycloaddition, forming a stable product. This was exemplified by the one-pot attachment of two molecular imaging moieties to a tumor binding cyclic peptide, and was extended to the conjugation of a DOTA chelator to a 12 kDa protein.
UR - http://www.scopus.com/inward/record.url?scp=84873673638&partnerID=8YFLogxK
U2 - 10.1039/c3cc38673b
DO - 10.1039/c3cc38673b
M3 - Journal article
C2 - 23370690
AN - SCOPUS:84873673638
SN - 1359-7345
VL - 49
SP - 1936
EP - 1938
JO - Chemical Communications
JF - Chemical Communications
IS - 19
ER -