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Oxaliplatin-Loaded Chitosan Nanoparticles Decorated with Cetuximab Single-Chain Variable Fragment for Human Colorectal Cancer Treatment.
Cell J
January 2025
Department of Medical Biotechnology, School of Advanced Technologies in Medicine, Tehran University of Medical Sciences, Tehran, Iran. Email:
Objective: Colorectal cancer (CRC) is the second leading cause of cancer-related deaths worldwide. Engineered biomolecules can be used as a targeted tool to deliver drugs directly to tumors that reduce the adverse effects of conventional treatments. We aimed to prepare non-targeted oxaliplatin-loaded chitosan nanoparticles (OXPT-CS NPs) and targeted OXPT-CS NPs decorated with cetuximab single-chain variable fragment (scFv) to send both NPs to epidermal growth factor receptor (EGFR) overexpressing HCT 116 cells, a human colorectal carcinoma cell line, for comparing their cytotoxicity.
View Article and Find Full Text PDFNaphtho[1,2-][1,4]diazepinedione-Based P2X4 Receptor Antagonists from Structure-Activity Relationship Studies toward PET Tracer Development.
J Med Chem
January 2025
European Institute for Molecular Imaging (EIMI), University of Muenster, Roentgenstr. 16, 48149 Muenster, Germany.
The P2X4 receptor is implicated in various pathological conditions, including neuropathic pain and cancer. This study reports the development of 1,4-naphthodiazepinedione-based P2X4 receptor antagonists aimed at both therapeutic applications and potential use as PET tracers for imaging P2X4 receptor expression in cancer. Structure-activity relationship studies aided by docking studies and molecular dynamics simulations led to a series of compounds with potent P2X4 receptor antagonism, promising inhibition of interleukin-1β release in THP-1 cells and suitability for radiolabeling with fluorine-18.
View Article and Find Full Text PDFCross-calibration of areal bone mineral densities and body composition between DMS Stratos and Hologic Horizon A dual-energy X-ray absorptiometers: The effect of body mass index.
J Clin Densitom
December 2024
Service de Médecine Nucléaire, Hôpital Lapeyronie, CHU Montpellier, France; Physiologie et Médecine Expérimentale du Cœur et des Muscles (PhyMedEx), INSERM, CNRS, Université de Montpellier (UM), France.
Purpose: The aim of this study was to investigate the correlations between areal bone mineral density (aBMD) and body composition measured by two dual-energy X-ray absorptiometers (DXA), the DMS Stratos® (STR) and the Hologic Horizon A® (HRZ), and then generate cross-calibration equations between the two scanners.
Methods: Repeat scans were obtained from 251 adults (85 % female), 36 ± 14 years old with mean body mass index (BMI) of 28.7 ± 11.
Thiosemicarbazone-Based Compounds: A Promising Scaffold for Developing Antibacterial, Antioxidant, and Anticancer Therapeutics.
Molecules
December 2024
Department of Pharmaceutical Chemistry, Drug Analyses and Radiopharmacy, Faculty of Pharmacy, Medical University of Lodz, 90-151 Lodz, Poland.
This paper presents the synthesis and characterization of new thiosemicarbazone derivatives with potential applications as antibacterial, antioxidant and anticancer agents. Six thiosemicarbazone derivatives (L-L5) were synthesized by reacting an appropriate thiosemicarbazide derivative with 2-pyridinecarboxaldehyde. The structures of the obtained compounds were confirmed using mass spectrometry, infrared spectroscopy, and NMR spectroscopy.
View Article and Find Full Text PDFPiperazine-based P2X4 receptor antagonists.
Arch Pharm (Weinheim)
January 2025
European Institute for Molecular Imaging (EIMI), University of Muenster, Muenster, Germany.
The P2X4 receptor (P2X4R), a ligand-gated ion channel activated by ATP, plays a critical role in neuroinflammation, chronic pain, and cancer progression, making it a promising therapeutic target. In this study, we explored the design and synthesis of piperazine-based P2X4R antagonists, building on the structural framework of paroxetine. A series of over 35 compounds were synthesized to investigate structure-activity relationships (SARs) in a Ca²⁺-flux assay for P2X4R antagonistic activity.
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