Current Topics in Medicinal Chemistry - Volume 12, Issue 23, 2012

Alpha-particles are of considerable growing interest for Targeted Alpha Therapy (TAT). TAT gains more attention as new targets, chemical labeling techniques and α-particle emitters are developed but translation of TAT into the clinic has been slow, in part because of the limited availability and the short physical half-lives of some of the available α- particle emitters. This article is an up-to-date overview of the literature concernin Read More

The successful application of OctreoScan® ([111In-DTPA]octreotide) in the diagnosis of sst2-expressing neuroendocrine tumors (NETs), on one hand, and the manifestation of peptide receptor targets in a wide range of human cancers, on the other, have synergistically induced a booming emergence of numerous radiolabeled peptide (radiopeptide) probes for tumor diagnosis and therapy in man. Definition of molecular tar Read More

For iodination (125/127I) of tyrosine-containing peptides, chloramin-T, Pre-Coated Iodo-Gen® tubes and Iodo- Beads® (Pierce) are commonly used for in vitro radioligand investigations and there have been reliant vendors hereof for decades. However, commercial availability of these radio-iodinated peptides is decreasing. For continuation of our research in this field we investigated and optimized (radio-)iodination of somato Read More

An overview how to measure and to quantify radiolysis by the addition of quenchers and to maintain Radio- Chemical Purity (RCP) of vulnerable methionine-containing regulatory peptides is presented. High RCP was only achieved with a combination of quenchers. However, quantification of RCP is not standardized, and therefore comparison of radiolabelling and RCP of regulatory peptides between different HPLC-systems and Read More

The paper focuses on the β-emitting radionuclides which might be useful for peptide receptor radionuclide therapy, PRRT. For the effective design of the radiopharmaceutical, the choice of radionuclide will depend on the purpose for which the radioligand is being used and on the physicochemical properties of the radionuclide. The important factor is also the availability and the cost of production. The physical char Read More

Dual-modality contrast agents, such as radiolabeled nanoparticles, are promising candidates for a number of diagnostic applications, since they combine the advantages of two different imaging modalities, namely SPECT or PET imaging with MR imaging. The benefit of such a combination is to more accurately interpret disease and abnormalities in vivo, by exploiting the advantages of each imaging technique, i.e. high sensitiv Read More