AI Article Synopsis
Article Abstract
Purpose: From a series of fluorinated analogues of puromycin, we recently identified [F]fluoroethylpuromycin (FEPURO) as a potential candidate for imaging the rate of protein synthesis in vivo. Herein, we describe the automation of the radiosynthesis, and evaluation of [F]FEPURO in vivo.
Procedures: [F]FEPURO was radiosynthesised in an automated module. PET imaging was conducted in Wistar rats under control and blocking conditions using the protein synthesis inhibitor cycloheximide. Biodistribution and metabolite studies at 30, 60 and 120 min were conducted in healthy rats.
Results: Automation of the radiosynthesis resulted in reduction of the synthesis time by half from the manual method. A steady increase in the SUV was observed in the time-activity curves for the whole brain as expected for a protein synthesis marker. However, rapid in vivo metabolism of [F]FEPURO within 15 min in plasma as well as the brain (4 % of parent 30 min p.i.) indicated formation of the [F]FET radio-metabolite in >90 % thus suggesting that observed increase in the brain uptake was due to the radiometabolite.
Conclusions: [F]FEPURO is not a suitable PET radiotracer for imaging protein synthesis rates in brain in vivo due to its rapid metabolism. Further structural modifications to prevent in vivo metabolism are underway.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/j.nucmedbio.2022.09.003 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Part II. Common questions and misconceptions about creatine supplementation: what does the scientific evidence really show?
J Int Soc Sports Nutr
December 2025
The Center for Applied Health Sciences, Canfield, OH, USA.
Creatine monohydrate supplementation (CrM) is a safe and effective intervention for improving certain aspects of sport, exercise performance, and health across the lifespan. Despite its evidence-based pedigree, several questions and misconceptions about CrM remain. To initially address some of these concerns, our group published a narrative review in 2021 discussing the scientific evidence as to whether CrM leads to water retention and fat accumulation, is a steroid, causes hair loss, dehydration or muscle cramping, adversely affects renal and liver function, and if CrM is safe and/or effective for children, adolescents, biological females, and older adults.
View Article and Find Full Text PDFExpanding the reaction toolbox for nanoscale direct-to-biology PROTAC synthesis and biological evaluation.
RSC Med Chem
December 2024
Modality Platform Technologies, GSK Stevenage SG1 2NY UK
High-throughput chemistry (HTC) and direct-to-biology (D2B) platforms allow for plate-based compound synthesis and biological evaluation of crude mixtures in cellular assays. The rise of these workflows has rapidly accelerated drug-discovery programs in the field of targeted protein degradation (TPD) in recent years by removing a key bottleneck of compound purification. However, the number of chemical transformations amenable to this methodology remain minimal, leading to limitations in the exploration of chemical space using existing library-based approaches.
View Article and Find Full Text PDFThe potential role of n-3 fatty acids and their lipid mediators on asthmatic airway inflammation.
Front Immunol
December 2024
School of Pharmacy, Changchun University of Traditional Chinese Medicine, Changchun, China.
Asthma, is a common, significant and diverse condition marked by persistent airway inflammation, with a major impact on human health worldwide. The predisposing factors for asthma are complex and widespread. The beneficial effects of omega-3 (n-3) polyunsaturated fatty acids (PUFAs) in asthma have increasingly attracted attention recently.
View Article and Find Full Text PDFRegulation of ubiquitination in sepsis: from PAMP versus DAMP to peripheral inflammation and cell death.
Front Immunol
December 2024
Department of Anesthesiology I, Meizhou People's Hospital, Meizhou, Guangdong, China.
Sepsis (sepsis) is a systemic inflammatory response triggered by infection, and its pathologic features include overproduction of peripheral inflammatory factors (e.g., IL-1β, IL-6, TNF-α), which ultimately leads to cytokine storm and multiple organ dysfunction syndrome (MODS).
View Article and Find Full Text PDFTherapeutic potential of 5-aminolevulinic acid in metabolic disorders: Current insights and future directions.
iScience
December 2024
Poltava State Medical University, Department of Pathophysiology, Poltava, Ukraine.
5-Aminolevulinic acid (5-ALA) is an essential compound in the biosynthesis of heme, playing a critical role in various physiological processes within the human body. This review provides the thorough analysis of the latest research on the molecular mechanisms and potential therapeutic benefits of 5-ALA in managing metabolic disorders. The ability of 5-ALA to influence immune response and inflammation, oxidative/nitrosative stress, antioxidant system, mitochondrial functions, as well as carbohydrate and lipid metabolism, is mediated by molecular mechanisms associated with the suppression of the transcription factor NF-κB signaling pathway, activation of the transcription factor Nrf2/heme oxygenase-1 (HO-1) system leading to the formation of heme-derived reaction products (carbon monoxide, ferrous iron, biliverdin, and bilirubin), which may contribute to HO-1-dependent cytoprotection through antioxidant and immunomodulatory effects.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!