Development of F-Labeled hydrophilic -cyclooctene as a bioorthogonal tool for PET probe construction.

Chem Commun (Camb)

Department of Radiology, Biomedical Research Imaging Center, and Lineberger Comprehensive Cancer Center, the University of North Carolina at Chapel Hill, Chapel Hill, North Carolina, 27599, USA.

Published: December 2023

We report the development of a hydrophilic F-labeled a-TCO derivative [F]3 (log  = 0.28) through a readily available precursor and a single-step radiofluorination reaction (RCY up to 52%). We demonstrated that [F]3 can be used to construct not only multiple small molecule/peptide-based PET agents, but protein/diabody-based imaging probes in parallel.

Download full-text PDF

Source
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC10785124PMC
http://dx.doi.org/10.1039/d3cc04212jDOI Listing

Publication Analysis

Top Keywords

development f-labeled
4
f-labeled hydrophilic
4
hydrophilic -cyclooctene
4
-cyclooctene bioorthogonal
4
bioorthogonal tool
4
tool pet
4
pet probe
4
probe construction
4
construction report
4
report development
4

Similar Publications

Histone deacetylase 6 (HDAC6) is an enzyme crucial in epigenetic regulation and protein degradation, with implications in various cancers and neurodegenerative disorders. While HDAC6 is recognized as a promising therapeutic target for Parkinson's and Alzheimer's diseases, its involvement in spinocerebellar ataxias (SCAs) remains underexplored. Currently, there are no direct methods available for characterizing HDAC6 in the brains of living subjects.

View Article and Find Full Text PDF

Selective PET imaging of CXCR4 using the AlF-labeled antagonist LY2510924.

Eur J Nucl Med Mol Imaging

December 2024

Radiopharmaceutical Research, Department of Pharmaceutical and Pharmacological Sciences, KU Leuven, Leuven, Belgium.

Background: [Ga]PentixaFor detects C-X-C chemokine receptor type 4 (CXCR4) overexpression in various malignancies, such as multiple myeloma and non-Hodgkin lymphomas, as well as in endocrine and inflammatory disorders. This study aimed to develop an AlF-labeled radiotracer derived from LY2510924 for CXCR4-targeted imaging, leveraging the physical and logistical advantages of fluorine-18.

Methods: We designed a CXCR4-specific radioprobe, [F]AlF-NOTA-SC, based on LY2510924 by incorporating a triglutamate linker and NOTA chelator to enable AlF-labeling.

View Article and Find Full Text PDF

[F]SF51 is a novel radioligand for imaging translocator protein 18 kDa (TSPO) that previously displayed excellent imaging properties in nonhuman primates. This study assessed its performance in human brain and its dosimetry. Seven healthy participants underwent brain PET imaging to measure TSPO binding using a two-tissue compartment model (2TCM) to calculate total distribution volume ().

View Article and Find Full Text PDF

Transmembrane protein 106B amyloid is a potential off-target molecule of tau PET tracers in the choroid plexus.

Nucl Med Biol

December 2024

Research Center for Accelerator and Radioisotope Science (RARiS), Tohoku University, Sendai, Japan; Graduate School of Pharmaceutical Science, Tohoku University, Sendai, Japan. Electronic address:

Purpose: Tau positron emission tomography (PET) has become an essential tool for the clinical diagnosis of neurodegenerative diseases and the study of tau pathology in the brain. However, some tau tracers exhibit off-target binding in the basal ganglia, choroid plexus, and meninges. Recently, transmembrane protein 106B (TMEM106B) was identified to form novel amyloid filaments in the brain during aging.

View Article and Find Full Text PDF

Glycogen synthase kinase 3 (GSK3) is a multifunctional serine/threonine kinase family that regulates diverse biological processes including glucose metabolism, insulin activity and energy homeostasis. Dysregulation of GSK3 is implicated in the development of several diseases such as type 2 diabetes mellitus, Alzheimer's disease (AD), and various cancer types. In this study, we report the synthesis and evaluation of a novel positron emission tomography (PET) ligand compound 28 (codenamed [F]GSK3-2209).

View Article and Find Full Text PDF

Want AI Summaries of new PubMed Abstracts delivered to your In-box?

Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!