Ultrastructural autoradiography showed high specific binding of (125I) triiodothyronine, as confirmed by a competition test, to plasma membranes, nuclei and mitochondria of human peripheral leukocytes. A high level of binding was also noted on the granulocytes' granules, especially in eosinophils.
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ACS Omega
December 2024
Heidelberg University, Medical Faculty Mannheim, Biomedical Chemistry, Theodor-Kutzer-Ufer 1-3, 68167 Mannheim, Germany.
By possibly bridging the gap between 2D cell assays and applications, tumor cell spheroid cultures offer promising avenues for advancing innovation in nuclear medicine. Regarding the evaluation of therapeutic radioligands, tumor cell spheroids have been successfully used to assess the therapeutic efficacy against human tumors. However, studies employing spheroids for testing diagnostic tracers are missing.
View Article and Find Full Text PDFBioorg Med Chem
February 2025
Department of Radiology, Washington University School of Medicine, St. Louis, MO 63110, United States. Electronic address:
The purinergic P2X ligand-gated ion channel 7 receptor (P2X7R) plays a critical role in various inflammatory processes and other diseases. Fast determination of compounds P2X7R binding potency and discovery of a promise PET radiotracer for imaging P2X7R require a P2X7R suitable radioligand for radioactive competitive binding assay. Herein, we designed and synthesized thirteen new P2X7R ligands and determined the in vitro binding potency.
View Article and Find Full Text PDFSci Transl Med
December 2024
Molecular Pharmacology, Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, Indianapolis, IN 46285, USA.
Orally bioavailable, synthetic nonpeptide agonists (NPAs) of the glucagon-like peptide-1 receptor (GLP-1R) may offer an effective, scalable pharmacotherapy to address the metabolic disease epidemic. One of the first molecules in the emerging class of GLP-1R NPAs is orforglipron, which is in clinical development for treating type 2 diabetes and obesity. Here, we characterized the pharmacological properties of orforglipron in comparison with peptide-based GLP-1R agonists and other NPAs.
View Article and Find Full Text PDFJ Pineal Res
November 2024
Faculty of Life Science and Technology, Kunming University of Science and Technology, Kunming, Yunnan, People's Republic of China.
The activation of melatonin receptors, belonging to the G-protein coupled receptors (GPCRs) superfamily, has been recognized as a vital approach in the clinical management of sleep disorders. Although the natural agonist melatonin and synthetic agonists (e.g.
View Article and Find Full Text PDFMol Pharm
January 2025
Division of Applied RI, Korea Institute of Radiological & Medical Sciences, Seoul 01812, Korea.
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