npj Imaging - A single-step radiolabeling strategy for PET, SPECT, and therapeutic radionuclides using nanoparticles as a universal chelator

Radiopharmaceuticals are a novel approach for tumor treatment, with several successful examples in the clinic. When developing this approach, the selection of the two radiometals for imaging and thera...

The radiohybrid (rh) concept to design targeted (and chemically identical) radiotracers for imaging or radionuclide therapy of tumors has gained momentum. For this strategy, a new bifunctional Silicon-based Fluoride Acceptor (SiFA) moiety (SiFA)SeFe was synthesized, endowed with improved hydrophilicity and high versatility of integration into rh-compounds. Preliminary radiolabeling and stability studies under different conditions were conducted using model bioconjugate peptides. Further, three somatostatin receptor 2 (sstR2)-targeted rh-compounds ((SiFA)SeFe-rhTATE1–3, TATE = (Tyr3)-octreotate) were developed. Compound (SiFA)SeFe-rhTATE3, enables labeling with 18F for PET imaging or chelation of 177Lu for therapy. The rh-compounds possess comparable receptor binding affinity and in vitro performance as good as the clinically proven gold standards. SstR2-specificity was further shown for (SiFA)SeFe-rhTATE2 using the chicken chorioallantoic membrane (CAM) model. The biodistribution of two compounds in mice showed high accumulation in tumors and excretion via the kidneys, demonstrating the clinical applicability of the (SiFA)SeFe moiety.

npj Imaging - A single-step radiolabeling strategy for PET, SPECT, and therapeutic radionuclides using nanoparticles as a universal chelator

Read the full paper: Development of a Highly Effective Bifunctional Ligand 2E-C-NETA for Targeted Lu-177 Therapy: Synthesis, Radiolabeling, In Vitro Stability, and In Vivo Biodistribution

The graphical abstract shows bacteriophages isolated against Ralstonia solanacearum that were radiolabeled with Tc-99m to trace their transport from soil to leaves. Optimized radiolabeling conditions...

Aryl iodides are privileged intermediates in organic synthesis, underpinning cross-coupling chemistry, late-stage functionalization, and radiolabeling in medicinal chemistry. However, regioselective arene iodination remains a challenge, as traditional electrophilic iodination methods often require harsh conditions, exhibit poor selectivity, or suffer from limited functional group tolerance and substrate scope. We report a rapid and regioselective arene iodination enabled by Lewis acid activation of N-iodosaccharin. Iron(III) chloride and silver(I) triflimide were found to catalyze the efficient iodination of a broad range of electron-rich arenes at room temperature. The method displayed broad functional group tolerance and was applicable to complex substrates, including natural products and pharmaceuticals. Furthermore, the iodination was found to be compatible with cross-coupling reactions, allowing one-pot halogenation and arylation sequences for direct access to biaryl compounds.

NOTA-AE105 is a GMP-grade PET ligand (purity ≥ 98.91%) for the urokinase-type plasminogen activator receptor (uPAR), optimized for ⁶⁴Cu or ⁶⁸Ga radiolabeling. Available for wholesale and retail; for laboratory research use only.（For wholesale prices, other specifications and uses, please consult our staff）

It's at times like this that the *real* value of ACSH makes itself known. Where else could you 1) Learn about the vileness of fruitcakes and 2) Simultaneously get a lesson on carbon-14 radiolabeling, ...

Complexation of radiometals by chelators allows for convenient radiolabeling of molecules of interest for the preparation of radiopharmaceuticals. In the chelator family, triazacyclononane (TACN)-base...