Aza-dibenzocyclooctynes for fast and efficient enzyme PEGylation via copper-free (3+2) cycloaddition.
A strained aza-dibenzocyclooctyne was prepared via a high-yielding synthetic route. Copper-free, strain-promoted click reaction with azides showed excellent kinetics, and a functionalised aza-cyclooctyne was applied in fast and efficient PEGylation of enzymes.
Debets
Marjoke F
MF
Institute for Molecules and Materials, Radboud University Nijmegen, Heyendaalseweg 135, NL-6525 AJ Nijmegen, The Netherlands.
van Berkel
Sander S
SS
Schoffelen
Sanne
S
Rutjes
Floris P J T
FP
van Hest
Jan C M
JC
van Delft
Floris L
FL
D001372:Aza Compounds / Q000737:chemistry*; D064026:Calbindins; D003300:Copper / Q000737:chemistry; D003516:Cycloparaffins / Q000737:chemistry*; D007700:Kinetics; D011092:Polyethylene Glycols / Q000737:chemistry*; D064030:S100 Calcium Binding Protein G / Q000737:chemistry*
D001372:Aza Compounds; D064026:Calbindins; D003516:Cycloparaffins; D064030:S100 Calcium Binding Protein G; D011092:Polyethylene Glycols; D003300:Copper