In vitro and in vivo evaluation of a 99mTc(I)-labeled bombesin analogue for imaging of gastrin releasing peptide receptor-positive tumors.
A new radiolabeled bombesin analogue, [99mTc(I)-PADA-AVA]bombesin (7-14), was synthesized and in vitro and in vivo characterized. High affinity and rapid internalization were obtained in binding assays. A specific binding towards gastrin releasing peptide receptors-positive tissues, pancreas and tumor, was observed in CD-1 nu/nu mice bearing PC-3 prostate adenocarcinoma xenografts. We therefore conclude that [99mTc(I)-PADA-AVA]bombesin (7-14) might have promising characteristics for applications in nuclear medicine, namely for diagnosis of GRP receptor overexpressing tumors.
La Bella
Roberto
R
Center for Radiopharmaceutical Science, Paul Scherrer Institute, CH-5232 Villigen, Switzerland. peter.blaeuenstein@psi.ch
Garcia-Garayoa
Elisa
E
Langer
Michael
M
Bläuenstein
Peter
P
Beck-Sickinger
Annette G
AG
Schubiger
P August
PA
D000230:Adenocarcinoma / Q000000981:diagnostic imaging* / Q000378:metabolism*; D001839:Bombesin / Q000031:analogs & derivatives / Q000138:chemical synthesis / Q000378:metabolism*; D006801:Humans; D008297:Male; D011471:Prostatic Neoplasms / Q000000981:diagnostic imaging* / Q000378:metabolism*; D011869:Radioligand Assay / Q000379:methods; D011877:Radionuclide Imaging; D019275:Radiopharmaceuticals / Q000138:chemical synthesis / Q000378:metabolism; D018004:Receptors, Bombesin / Q000378:metabolism*; D015203:Reproducibility of Results; D012680:Sensitivity and Specificity; D017556:Technetium Compounds / Q000138:chemical synthesis / Q000378:metabolism; D014018:Tissue Distribution; D014407:Tumor Cells, Cultured / Q000000981:diagnostic imaging / Q000378:metabolism
D019275:Radiopharmaceuticals; D018004:Receptors, Bombesin; D017556:Technetium Compounds; D001839:Bombesin