Radioactively labeled compounds are important for use as imaging probes or radiotherapeutic agents. Most radioisotopes with suitable decay properties are transition metals or elements with metallic character. Therefore, bifunctional chelators are required for stable tethering of a given radionuclide to targeted biomolecules.
However, preparing such multifunctional radioconjugates by conventional synthetic means is a significant challenge. To address this, a collaboration led by Thomas Mindt at University Hospital Basel and the University of Basel in Switzerland applied click chemistry toward the efficient assembly of conjugates containing a 99mTc-based SPECT probe and two different biochemical entities, and their work is reported in ChemMedChem.
Starting from azide-functionalized biomolecules and readily available alkyne pro-chelators derived from amino acids, Mindt and colleagues assembled multifunctional conjugates by convenient one-pot procedures without the need for protecting groups. They applied this copper(I)-catalyzed alkyne–azide cycloaddition (CuAAC) methodology to the preparation of a 99mTc-labeled conjugate comprising a tumor-targeting peptide sequence (bombesin(7–14)) and a low-molecular-weight albumin binder (a pharmacological modifier that prolongs the conjugate's blood circulation lifetime).
The possibility of selectively combining two different groups with biological function and a metal chelating system in a single step is a very attractive feature for the development of metallic radiotracers and opens numerous applications with great potential, including the design of radiopharmaceuticals with improved biological characteristics, multimodality imaging probes, bivalent or bi-specific targeting agents, and conjugates useful for combination therapies.
Author: Thomas Mindt, Universität / Universitätsspital Basel (Switzerland),
Title: Molecular Assembly of Multifunctional 99mTc Radiopharmaceuticals Using "Clickable" Amino Acid Derivatives
ChemMedChem, Permalink to the article: http://dx.doi.org/10.1002/cmdc.201000342
A Map of the Cell’s Power Station
18.08.2017 | Albert-Ludwigs-Universität Freiburg im Breisgau
On the way to developing a new active ingredient against chronic infections
18.08.2017 | Deutsches Zentrum für Infektionsforschung
Whether you call it effervescent, fizzy, or sparkling, carbonated water is making a comeback as a beverage. Aside from quenching thirst, researchers at the University of Illinois at Urbana-Champaign have discovered a new use for these "bubbly" concoctions that will have major impact on the manufacturer of the world's thinnest, flattest, and one most useful materials -- graphene.
As graphene's popularity grows as an advanced "wonder" material, the speed and quality at which it can be manufactured will be paramount. With that in mind,...
Physicists at the University of Bonn have managed to create optical hollows and more complex patterns into which the light of a Bose-Einstein condensate flows. The creation of such highly low-loss structures for light is a prerequisite for complex light circuits, such as for quantum information processing for a new generation of computers. The researchers are now presenting their results in the journal Nature Photonics.
Light particles (photons) occur as tiny, indivisible portions. Many thousands of these light portions can be merged to form a single super-photon if they are...
For the first time, scientists have shown that circular RNA is linked to brain function. When a RNA molecule called Cdr1as was deleted from the genome of mice, the animals had problems filtering out unnecessary information – like patients suffering from neuropsychiatric disorders.
While hundreds of circular RNAs (circRNAs) are abundant in mammalian brains, one big question has remained unanswered: What are they actually good for? In the...
An experimental small satellite has successfully collected and delivered data on a key measurement for predicting changes in Earth's climate.
The Radiometer Assessment using Vertically Aligned Nanotubes (RAVAN) CubeSat was launched into low-Earth orbit on Nov. 11, 2016, in order to test new...
A study led by scientists of the Max Planck Institute for the Structure and Dynamics of Matter (MPSD) at the Center for Free-Electron Laser Science in Hamburg presents evidence of the coexistence of superconductivity and “charge-density-waves” in compounds of the poorly-studied family of bismuthates. This observation opens up new perspectives for a deeper understanding of the phenomenon of high-temperature superconductivity, a topic which is at the core of condensed matter research since more than 30 years. The paper by Nicoletti et al has been published in the PNAS.
Since the beginning of the 20th century, superconductivity had been observed in some metals at temperatures only a few degrees above the absolute zero (minus...
16.08.2017 | Event News
04.08.2017 | Event News
26.07.2017 | Event News
18.08.2017 | Life Sciences
18.08.2017 | Physics and Astronomy
18.08.2017 | Materials Sciences