Simple and convenient radiolabeling of proteins using a prelabeling-approach with thiol-DOTA.
Commonly applied methods for radiometal-labeling of proteins require complex and protracted derivatization reactions of the protein and the subsequent radiolabeling is time-consuming due to the low reaction temperatures applicable. Therefore, a convenient and efficient prelabeling technique for proteins using the DOTA derivative 2,2',2''-(10-(2-(2-mercaptoethylamino)-2-oxoethyl)-1,4,7,10-tetraazacyclododecane-1,4,7-triyl)triacetic acid (thiol-DOTA) containing a thiol moiety for rapid and selective introduction into maleimide-derivatized proteins was developed. Thiol-DOTA was labeled with (68)Ga, (90)Y and (177)Lu and subsequently introduced into bovine serum albumin and a human IgG with maximum radiochemical yields of 66%. The entire radiolabeling procedure was completed after only 30 min making this a favorable new labeling technique for proteins.
Wängler
Carmen
C
McConnell Brain Imaging Center, Montreal Neurological Institute, McGill University, University Street 3800, Montreal H3A 2B4, Quebec, Canada. carmen.waengler@med.uni-muenchen.de
Schirrmacher
Ralf
R
Bartenstein
Peter
P
Wängler
Björn
B
D000818:Animals; D002417:Cattle; D006573:Heterocyclic Compounds, 1-Ring / Q000737:chemistry*; D006801:Humans; D007074:Immunoglobulin G / Q000737:chemistry; D007553:Isotope Labeling / Q000379:methods*; D008301:Maleimides / Q000737:chemistry; D008670:Metals / Q000138:chemical synthesis / Q000737:chemistry; D011506:Proteins / Q000737:chemistry*; D012710:Serum Albumin, Bovine / Q000737:chemistry
C541279:2,2',2''-(10-(2-(2-mercaptoethylamino)-2-oxoethyl)-1,4,7,10-tetraazacyclododecane-1,4,7-triyl)triacetic acid; D006573:Heterocyclic Compounds, 1-Ring; D007074:Immunoglobulin G; D008301:Maleimides; D008670:Metals; D011506:Proteins; C043592:maleimide; D012710:Serum Albumin, Bovine