In vivo somatostatin receptor scintigraphy is a valuable method for the visualization of human endocrine tumors and their metastases. In fact, peptide ligands of somatostatin receptors (sst's) conjugated with chelating agents are in clinical use. We have recently developed octreotide dicarba-analogs, which show interesting binding profiles at sst's. In this context, it was mandatory to explore ...

UNLABELLED Multistep immune targeting holds great promise for radioimmunodiagnosis and therapy of cancer. Pretargeting of the tetrameric single-chain, variable-fragment streptavidin construct of the tetrameric monoclonal antibody CC49 with subsequent administration of radiolabeled 1,4,7,10-tetraazacyclododecane-N,N',N'',N'''-tetraacetic acid (DOTA)-biotin has yielded promising results in TAG-72...

We classify the discontinuity of loss in both five-param and eight-param rotated object detection methods as rotation sensitivity error (RSE) which will result performance degeneration. introduce a novel modulated to alleviate problem network (RSDet) consists an single-stage detector loss. Our proposed RSDet has several advantages: 1) it reformulates predicting corners objects while most previo...

The thesis is focused on site-specific labeling of affinity molecules for different applications where two types of binding proteins, Affibody molecules and antibodies, have been used. For the purpose of improving the properties of Affibody molecules for in vivo imaging, novel bifunctional chelators for radiolabeling using the radionuclide 111In were evaluated. In a first study, two chelators d...

introduction: bombesin is a 14-aminoacid peptide isolated from frog skin. the mammalian counterparts of the frog peptide are neuromedin b (nmb) and gastrin-releasing peptide (grp). bombesin (bbn) is a peptide showing high affinity for the gastrin releasing peptide receptor (grpr). prostate, small cell lung cancer, breast, gastric, and colon cancers are known to over express receptors to bombesi...

The development of novel protein-targeted MRI contrast agents crucially depends on the ability to derivatise suitable targeting moieties with a high payload of relaxation enhancer (e.g., gadolinium(iii) complexes such as Gd-DOTA), without losing affinity for the target proteins. Here, we report robust synthetic procedures for the preparation of trivalent Gd-DOTA reagents with various chemical h...

We report our initial investigations into the use of tetraazamacrocycles as zirconium-89 chelators. We describe the synthesis and complete characterization of several Zr tetraazamacrocycle complexes, and definitively describe the first crystal structure of zirconium 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (Zr-DOTA) using single crystal X-ray diffraction analysis. After evaluati...

The design and synthesis of a phthalocyanine--Gd-DOTA conjugate is presented to open the way to novel molecular theranostics, combining the properties of MRI contrast imaging with photodynamic therapy. The rational design of the conjugate integrates isomeric purity of the phthalocyanine core substitution, suitable biocompatibility with the use of polyoxo water-solubilizing substituents, and a c...

In this issue of The Journal of Nuclear Medicine, Gabriel et al. (1) report their experience with 68Ga-labeled 1,4,7,10tetraazacyclododecane-N,N9,N99,N999tetraacetic acid-D-Phe1-Tyr3-octreotide (68Ga-DOTA-TOC) PET in a series of 84 patients with neuroendocrine tumors (NET). PET was more accurate with a higher detection rate than somatostatin receptor scintigraphy (using 111In-DOTA-TOC or 99mTc-...