The potential of targeted therapy with radiolabeled peptides has been reported in several clinical trials. Although there have been many improvements in dose estimation, a general and reliable dosimetric approach in peptide receptor radionuclide therapy (PRRT) is still a matter of debate. This article reviews the methods for PRRT dosimetry and the results presented in the literature. Radiopharm...

UNLABELLED Radiolabeled bombesin (BBN) analogs that bind to the gastrin-releasing peptide receptor (GRPR) represent a topic of active investigation for the development of molecular probes for PET or SPECT of prostate cancer (PCa). RM1 and AMBA have been identified as the 2 most promising BBN peptides for GRPR-targeted cancer imaging and therapy. In this study, to develop a clinically translatab...

In this issue of The Journal of Nuclear Medicine, Wild et al. report the binding and animal biodistribution data of [Lys(Ahx-DTPA-In)NH2]exendin-4 (Ahx is aminohexanoic acid; DTPA is diethylenetriaminepentaacetic acid), an analog of glucagonlike peptide-1 (GLP-1) (1). Their results raise high hopes of actually achieving selective and potent receptormediated targeting of tumors with a radiolabel...

The arginine-glycine-aspartic acid (RGD) cell adhesion motif was discovered in fibronectin by Pierschbacher and Ruoslahti 20 years ago (1). Shortly thereafter, Smith and Cheresh (2) identified the vitronectin receptor, or v 3 integrin, as one of the adhesion molecules recognizing this sequence. The v 3 integrin is expressed on the luminal surface of neovasculature but is not found on the endoth...

Cytotoxicity was induced in cells mimicking SARS-CoV-2 infection by a 225 Ac-radiolabeled antibody that targets the RBD2 of spike protein.

OBJECTIVES Cancer has been investigated using various pre-targeting techniques or models focusing on radiobombesin analogues; however, both are not offered together. In this study, nano-bombesin labeling by a pre-targeting system was undertaken to develop an alternative approach for prostate tumor treatment. METHODS A two-step pre-targeting system utilizing a combination of streptavidin (SA),...

OBJECTIVES Our aim was to image angiogenesis produced by endomyocardial injection of phVEGF165 in a swine model of hibernating myocardium using [123I]Gluco-arginine-glycine-aspartic acid (RGD) targeting the alphavbeta3 integrins. BACKGROUND A noninvasive test to monitor the efficacy of therapy inducing angiogenesis is needed. The interaction between extracellular matrix and endothelial cells ...

The integrin family is a group of transmembrane glycoprotein comprised of 19 α- and 8 β-subunits that are expressed in 25 different α/β heterodimeric combinations on the cell surface. Integrins play critical roles in many physiological processes, including cell attachment, proliferation, bone remodeling, and wound healing. Integrins also contribute to pathological events such as thrombosis, ath...

Arginine-glycine-aspartic acid (RGD) peptides preferentially bind to alphavbeta3 integrin, an integrin expressed on newly formed endothelial cells and on various tumor cells. When labeled with beta-emitting radionuclides, these peptides can be used for peptide-receptor radionuclide therapy of malignant tumors. These studies aimed to investigate whether tumor targeting and tumor therapy could be...

The role in platelet function of the cell-binding region of fibronectin was explored by the use of synthetic peptides. The prototypical peptide gly-arg-gly-asp-ser was capable of inhibiting thrombin-induced platelet aggregation without altering the degree of platelet activation as judged by the secretion of 14C-serotonin. The peptide also effectively inhibited, in a concentration-dependent mann...