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http://dx.doi.org/10.1111/j.1365-2125.1975.tb00561.x | DOI Listing |
Langmuir
January 2025
Gordon Center for Medical Imaging, Department of Radiology, Massachusetts General Hospital and Harvard Medical School, Boston, Massachusetts 02114, United States.
Nanocarriers have shown significant promise in the diagnosis and treatment of various diseases, utilizing a wide range of biocompatible materials such as metals, inorganic substances, and organic components. Despite diverse design strategies, key physicochemical properties, including hydrodynamic diameter, shape, surface charge, and hydrophilicity/lipophilicity, are crucial for optimizing biodistribution, pharmacokinetics, and therapeutic efficacy. However, these properties are often influenced by drug payload, presenting an ongoing challenge in developing versatile platform technologies for theranostics.
View Article and Find Full Text PDFJ Med Chem
January 2025
Department of Medicinal Chemistry, University of Minnesota, 308 Harvard Street SE, Minneapolis, Minnesota 55455, United States.
The antibacterial agent Bio-AMS is metabolized in vivo through hydrolysis of the central acyl-sulfamide linker leading to high clearance and release of a moderately cytotoxic metabolite . Herein, we disclose analogues designed to prevent the metabolism of the central acyl-sulfamide moiety through steric hindrance or attenuation of the acyl-sulfamide electrophilicity. was identified as a metabolically stable analogue with a single-digit nanomolar dissociation constant for biotin protein ligase (BPL) and minimum inhibitory concentrations (MICs) against and ranging from 0.
View Article and Find Full Text PDFAm J Transl Res
December 2024
Department of Pharmacy, The Fourth Hospital of Hebei Medical University Shijiazhuang 050000, Hebei, China.
Objectives: The aim of this study was to establish an ultra-performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS) method for the detection of osimertinib in rat plasma, lung and brain tissues.
Methods: Forty-eight rats were randomly divided into an experimental group (receiving osimertinib at doses of 5, 8, and 10 mg/kg) and a control group. After continuous intragastric administration for 15 days, samples of blood, lung, and brain tissue were collected.
Clin Transl Sci
January 2025
Division of Pharmacotherapy and Experimental Therapeutics, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, North Carolina, USA.
In neurovascular settings, including treatment and prevention of ischemic stroke and prevention of thromboembolic complications after percutaneous neurointerventional procedures, dual antiplatelet therapy with a P2Y12 inhibitor and aspirin is the standard of care. Clopidogrel remains the most commonly prescribed P2Y12 inhibitor for neurovascular indications. However, patients carrying CYP2C19 no-function alleles have diminished capacity for inhibition of platelet reactivity due to reduced formation of clopidogrel's active metabolite.
View Article and Find Full Text PDFRapid Commun Mass Spectrom
April 2025
Camel Forensic Laboratory, Central Veterinary Research Laboratory, Dubai, UAE.
Rationale: LGD-4033, a selective androgen receptor modulator (SARM), is recognized for promoting muscle growth and enhancing athletic performance. Its potent anabolic effects have led to its prohibition in both human and animal sports. Although initial in vitro studies have offered insights into its metabolism, an in-depth in vivo analysis is necessary to fully understand its metabolic pathways.
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