Triphenylphosphonium-fluorochromes (TPP-fluorochromes) are a new class of spectrally variable, mitochondrially targeted probes, with an [(18)F] labeling option which, when enabled, allows imaging of a cardiac perfusion deficit using PET/CT.
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http://dx.doi.org/10.1039/c3cc45802d | DOI Listing |
Respir Res
January 2025
Division of Allergy, Pulmonary and Critical Care Medicine, Department of Medicine, School of Medicine and Public Health, University of Wisconsin-Madison, 600 Highland Avenue, Madison, WI, 53792, USA.
Progressive forms of interstitial lung diseases, including idiopathic pulmonary fibrosis (IPF), are deadly disorders lacking non-invasive biomarkers for assessment of early disease activity, which presents a major obstacle in disease management. Excessive extracellular matrix (ECM) deposition is a hallmark of these disorders, with fibronectin being an abundant ECM glycoprotein that is highly upregulated in early fibrosis and serves as a scaffold for the deposition of other matrix proteins. Due to its role in active fibrosis, we are targeting fibronectin as a biomarker of early lung fibrosis disease activity via the PEGylated fibronectin-binding polypeptide (PEG-FUD).
View Article and Find Full Text PDFACS Chem Biol
January 2025
Department of Chemistry, University of Florida, Gainesville Florida 32611, United States.
Small molecules are essential for investigating the pharmacology of membrane proteins and remain the most common approach for therapeutically targeting them. However, most experimental small molecule screening methods require ligands containing radiolabels or fluorescent labels and often involve isolating proteins from their cellular environment. Additionally, most conventional screening methods are suited for identifying compounds with moderate to higher affinities ( < 1 μM) and are less effective at detecting lower affinity compounds, such as weakly binding molecular fragments.
View Article and Find Full Text PDFNaunyn Schmiedebergs Arch Pharmacol
January 2025
Obstetrics and Gynecology Department, Tehran University of Medical Sciences, Tehran, Iran.
Breast cancer is the most frequent non-dermatologic malignancy in women. Breast cancer is characterized by the expression of the human epidermal growth factor receptor type 2 (HER2), and the presence or lack of estrogen receptor (ER) and progesterone receptor (PR) expression. HER2 overexpression is reported in about 20 to 25% of breast cancer patients, which is usually linked to cancer progression, metastases, and poor survival.
View Article and Find Full Text PDFChemMedChem
December 2024
Department of Pharmaceutical and Medicinal Chemistry, Christian-Albrechts-University of Kiel, Gutenbergstr. 76, 24118, Kiel, Germany.
Inhibitors of ʟ-lactate transport are in development as a novel mode of action in antitumor therapy and malaria. Previously, we used radiolabeled ʟ-lactate to assay transport via the human monocarboxylate transporter 1, MCT1, and the structurally unrelated malaria parasite's transporter, PfFNT. We encountered a sensitivity limit at IC around 100 nM possibly resulting from the required high cell number per sample.
View Article and Find Full Text PDFActa Histochem
December 2024
Department of Pharmacology and Toxicology, National Institute of Pharmaceutical Education and Research (NIPER)-Ahmedabad, Gandhinagar, Gujarat 382355, India. Electronic address:
Vascular endothelial cells (VECs) play a crucial role in the development and maintenance of vascular biology specific to the tissue types. Molecular signature-based labeling and imaging of VECs help researchers understand potential mechanisms linking VECs to disease pathology, serving as valuable biomarkers in clinical settings and trials. Labeling techniques involve selectively tagging or marking VECs for visualization.
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