TY - JOUR
T1 - General method to label antisense oligonucleotides with radioactive halogens for pharmacological and imaging studies
AU - Kühnast, B.
AU - Dollé, F.
AU - Terrazzino, S.
AU - Rousseau, B.
AU - Loc'h, C.
AU - Vaufrey, F.
AU - Hinnen, F.
AU - Doignon, I.
AU - Pillon, F.
AU - David, C.
AU - Crouzel, C.
AU - Tavitian, B.
PY - 2000
Y1 - 2000
N2 - Evaluation of oligonucleotides for biomedical applications requires different in vivo and in vitro approaches (pharmacokinetics, biodistribution, macro- and microimaging, metabolism, ...), that are performed with different radioisotopes according to the temporal and spatial resolution needed. A method to introduce radioactive isotopes of halogens (fluorine, bromine, and iodine) in a small and stable molecule has been developed. Radiosynthons can then be conjugated with any given oligonucleotide in one step to create the appropriate radiotracer. This general radiolabeling procedure for oligonucleotides is efficient to synthesize 18F-, 76Br-, and 125I-oligonucleotides for biological needs. Applications of the method to biodistribution, metabolism, in vivo and ex vivo imaging of 125I- and 18F-labeled oligonucleotides are reported.
AB - Evaluation of oligonucleotides for biomedical applications requires different in vivo and in vitro approaches (pharmacokinetics, biodistribution, macro- and microimaging, metabolism, ...), that are performed with different radioisotopes according to the temporal and spatial resolution needed. A method to introduce radioactive isotopes of halogens (fluorine, bromine, and iodine) in a small and stable molecule has been developed. Radiosynthons can then be conjugated with any given oligonucleotide in one step to create the appropriate radiotracer. This general radiolabeling procedure for oligonucleotides is efficient to synthesize 18F-, 76Br-, and 125I-oligonucleotides for biological needs. Applications of the method to biodistribution, metabolism, in vivo and ex vivo imaging of 125I- and 18F-labeled oligonucleotides are reported.
UR - http://www.scopus.com/inward/record.url?scp=0033794909&partnerID=8YFLogxK
U2 - 10.1021/bc990183i
DO - 10.1021/bc990183i
M3 - Article
SN - 1043-1802
VL - 11
SP - 627
EP - 636
JO - Bioconjugate Chemistry
JF - Bioconjugate Chemistry
IS - 5
ER -