(89)Zr-based imaging agents hold great promise as novel radio-tracers in nuclear medicine. However, insufficient stability of currently used radiometal complexes in vivo is a safety concern for clinical applications. We herein report the first octadentate bifunctional chelating agent for the development of (89)Zr-labelled (bio)conjugates with improved stability.
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http://dx.doi.org/10.1039/c4cc05558f | DOI Listing |
EJNMMI Radiopharm Chem
May 2024
Department of Radiopharmaceutical, IRCCS Sacro Cuore Don Calabria Hospital, Via Don A. Sempreboni 5, 37024, Negrar di Valpolicella, Verona, Italy.
Background: Positron emission tomography (PET) is a highly sensitive method that provides fine resolution images, useful in the field of clinical diagnostics. In this context, Zirconium-89 (Zr)-based imaging agents have represented a great challenge in molecular imaging with immuno-PET, which employs antibodies (mAbs) as biological vectors. Indeed, immuno-PET requires radionuclides that can be attached to the mAb to provide stable in vivo conjugates, and for this purpose, the radioactive element should have a decay half-life compatible with the time needed for the biodistribution of the immunoglobulin.
View Article and Find Full Text PDFInorg Chem
December 2023
Department of Chemistry, College of Arts and Science, University of Saskatchewan, 110 Science Place, Saskatoon, Saskatchewan S7N-5C9, Canada.
Zirconium-89-labeled monoclonal antibodies and other large macromolecules such as nanoparticles hold great promise as positron emission tomography imaging agents. In general, zirconium-89 is an ideal radionuclide for long-circulating vectors such as antibodies or nanoparticles. It is also a promising radionuclide for theranostic radiopharmaceuticals due to its suitable match in half-life with actinium-225, thorium-227, lutetium-177, and others.
View Article and Find Full Text PDFInorg Chem
December 2023
Ph.D. Program in Chemistry, The Graduate Center of the City University of New York, New York, New York10016, United States.
Three isotopes of scandium─Sc, Sc, and Sc─have attracted increasing attention as potential candidates for use in imaging and therapy, respectively, as well as for possible theranostic use as an elementally matched pair. Here, we present the octadentate chelator 3,4,3-(LI-1,2-HOPO) (or HOPO), an effective chelator for hard cations, as a potential ligand for use in radioscandium constructs with simple radiolabeling under mild conditions. HOPO forms a 1:1 Sc-HOPO complex that was fully characterized, both experimentally and theoretically.
View Article and Find Full Text PDFChemMedChem
August 2020
Universität Heidelberg, Anorganisch-Chemisches Institut, Neuenheimer Feld 270, 69120, Heidelberg, Germany.
Hepta- and octadentate bispidines (3,7-diazabicyclo[3.3.1]nonane, diaza-adamantane) with acetate, methyl-pyridine, and methyl-picolinate pendant groups at the amine donors of the bispidine platform have been prepared and used to investigate Bi coordination chemistry.
View Article and Find Full Text PDFDalton Trans
June 2020
Medicinal Inorganic Chemistry Group, Department of Chemistry, University of British Columbia, 2036 Main Mall, Vancouver, British Columbia V6T 1Z1, Canada.
The peptide is an important class of biological targeting molecule; herein, a new bifunctional octadentate non-macrocyclic H4octapa, tBu4octapa-alkyl-NHS, which is compatible with solid-phase peptide synthesis and thus useful for radiopeptide preparation, has been synthesized. To preserve denticity, the alkyl-N-hydroxylsuccinimide linker was covalently attached to the methylene-carbon on one of the acetate arms, yielding a chiral carbon center. According to density-functional theory (DFT) calculations using [Lu(octapa-alkyl-benzyl-ester)]- as a simulation model, the chirality has minimal effects on the complex geometry; regardless of the S-/R-stereochemistry, DFT calculations revealed two possible geometric isomers, distorted bicapped trigonal antiprism (DBTA) and distorted square antiprism (DSA), due to the asymmetry in the chelator.
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