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Design, synthesis, and biological evaluation of novel thiourea derivatives as small molecule inhibitors for prostate specific membrane antigen.
Bioorg Chem
January 2025
Department of Chemistry, Indian Institute of Technology Indore, Indore 453552 India; Department of Biosciences and Biomedical Engineering, Indian Institute of Technology Indore, Indore 453552 India. Electronic address:
Prostate cancer (PCa) has emerged to be the second leading cause of cancer-related deaths in men. Molecular imaging of PCa using targeted radiopharmaceuticals specifically to PCa cells promises accurate staging of primary disease, detection of localized and metastasized tumours, and helps predict the progression of the disease. Glutamate urea heterodimers have been popularly used as high-affinity small molecules in the binding pockets of popular and well-characterized PCa biomarker, prostate specific membrane antigen (PSMA).
View Article and Find Full Text PDFTc-DTPA-Collagen Radiotracer for the Noninvasive Detection of Infective Endocarditis.
ACS Infect Dis
January 2025
Unidad de Medicina y Cirugía Experimental, Hospital General Universitario Gregorio Marañón, Instituto de Investigación Sanitaria Gregorio Marañón (IiSGM), 28007 Madrid, Spain.
Infective endocarditis (IE) represents a significant concern among hospital-acquired infections, frequently caused by the Gram-positive bacterium . Nuclear imaging is emerging as a noninvasive and precise diagnostic tool. However, the gold standard radiotracer [F]-FDG cannot distinguish between infection and inflammation, resulting in false positives.
View Article and Find Full Text PDFTc-Labeled D-Type PTP as a Plectin-Targeting Single-Photon Emission Computed Tomography Probe for Hepatocellular Carcinoma Imaging.
Bioconjug Chem
December 2024
Department of Nuclear Medicine, Shanghai General Hospital, Shanghai Jiao Tong University School of Medicine, Shanghai 200080, China.
Plectin, a scaffolding protein overexpressed in tumor cells, plays a significant role in hepatocellular carcinoma (HCC) proliferation, invasion, and migration. However, the use of L-type peptides for targeting plectin is hindered by their limited stability and retention. We designed a D-type plectin-targeting peptide (PTP) and developed a novel single-photon emission computed tomography (SPECT) probe for HCC imaging.
View Article and Find Full Text PDFFirst-in-human study of Tc-labeled fucoidan, a SPECT tracer targeting P-selectin.
EJNMMI Res
November 2024
Department of Vascular Medicine, Amsterdam Cardiovascular Sciences, Amsterdam UMC, University of Amsterdam, Amsterdam, The Netherlands.
Article Synopsis
- The study focuses on Tc-fucoidan, a compound derived from brown algae, which targets P-selectin for early identification of thrombosis.
- In the safety assessment involving ten healthy volunteers, Tc-fucoidan was well tolerated with no adverse effects and demonstrated reliable uptake in human thrombi in gamma counting experiments.
- Although the results showed potential for imaging thrombi in certain cases, the overall findings do not support further clinical use of Tc-fucoidan for diagnosing deep vein thrombosis (DVT), suggesting exploration of alternative P-selectin tracers instead.
Development of a Novel Tc-Labeled Folate Derivative Containing Phenyl Isonitrile to Target Folate Receptor with Reduced Renal Uptake.
Mol Pharm
November 2024
Key Laboratory of Radiopharmaceuticals of the Ministry of Education, NMPA Key Laboratory for Research and Evaluation of Radiopharmaceuticals (National Medical Products Administration), College of Chemistry, Beijing Normal University, Beijing 100875, PR China.
The folate receptor has attracted much attention in the field of radiolabeled imaging agents due to the significant difference in its expression levels between tumor cells and most normal cells. However, the development of folate-based imaging agents has been limited by their high uptake in the kidney. In this study, to reduce the high renal uptake of radiolabeled folate-based tracers, a phenyl-isonitrile folate derivative (CNMBFA) was designed and labeled with technetium-99m.
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