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Development of [¹⁸F]Maleimide-Based Glycogen Synthase Kinase-3β Ligands for Positron Emission Tomography Imaging.

ABSTRACT: Dysregulation of glycogen synthase kinase-3β (GSK-3β) is implicated in the pathogenesis of neurodegenerative and psychiatric disorders. Thus, development of GSK-3β radiotracers for positron emission tomography (PET) imaging is of paramount importance, because such a noninvasive imaging technique would allow better understanding of the link between the activity of GSK-3β and central nervous system disorders in living organisms, and it would enable early detection of the enzyme's aberrant activity. Herein, we report the synthesis and biological evaluation of a series of fluorine-substituted maleimide derivatives that are high-affinity GSK-3β inhibitors. Radiosynthesis of a potential GSK-3β tracer [¹⁸F]10a is achieved. Preliminary in vivo PET imaging studies in rodents show moderate brain uptake, although no saturable binding was observed in the brain. Further refinement of the lead scaffold to develop potent [¹⁸F]-labeled GSK-3 radiotracers for PET imaging of the central nervous system is warranted.

SUBMITTER: Hu K

PROVIDER: S-EPMC5346984 | biostudies-literature |

REPOSITORIES: biostudies-literature

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18F-flutemetamol positron emission tomography in cardiac amyloidosis.

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| S-EPMC8993783 | biostudies-literature

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| S-EPMC8709812 | biostudies-literature

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| S-EPMC8616877 | biostudies-literature

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| S-EPMC8648691 | biostudies-literature

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Normal imaging findings after aortic valve implantation on 18F-Fluorodeoxyglucose positron emission tomography with computed tomography.

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| S-EPMC8648629 | biostudies-literature

18F-Fluorodeoxyglucose Positron Emission Tomography and Computed Tomography With Magnetic Resonance for Diagnosing Adult-Onset Still's Disease.

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| S-EPMC7649810 | biostudies-literature

18F-fluorodeoxyglucose-positron emission tomography/computed tomography for the diagnosis of polymyalgia-like illnesses: a retrospective study.

Project description:BackgroundVarious inflammatory conditions may present with musculoskeletal symptoms similar to those of polymyalgia rheumatica (PMR). We investigated findings on 18F-fluorodexoxyglucose (FDG)-positron emission tomography/computed tomography (PET/CT) images that may differentiate PMR from polymyalgia-like illnesses.MethodsWe analyzed data from 25 patients with new-onset polymyalgia-like illnesses who fulfilled Bird's diagnostic criteria for PMR and had undergone FDG-PET/CT scan. To assess the uptake by major joints and synovial bursae, particularly at PMR-specific sites (shoulder, sternoclavicular, and hip joints, interspinous bursae, ischial tuberosities, and greater trochanters), we used visual scoring system to score FDG uptake: 0, no uptake (same as bone); 1, slight uptake; 2, moderate uptake (same as the liver); 3, greater uptake than the liver; and 4, uptake as strong as in the cerebellum.ResultsThe final diagnoses were PMR in 17 patients and non-PMR in eight patients (three malignancies, two infections, one cholesterol crystal embolism, one ANCA-associated vasculitis, and one undefined diagnosis). Although the serum MMP-3 levels were significantly higher in patients with PMR, C-reactive protein and erythrocyte sedimentation rate mean values did not differ between the two groups. In PMR-specific sites, FDG accumulations were observed in all cases of PMR, with a high PET-positive score of 2.00 (range, 0-3), but it was low in non-PMR cases, with a PET-positive score of 1.00 (range, 0-3).ConclusionsThe FDG accumulation patterns in polymyalgia-like illness differ from those in PMR, despite the similar clinical presentations of both conditions. An FDG-PET/CT scan is useful for differentiating PMR from other polymyalgia-like illnesses.

| S-EPMC7181584 | biostudies-literature

Breast Cancer Subtype Prediction Model Employing Artificial Neural Network and 18F-Fluorodeoxyglucose Positron Emission Tomography/ Computed Tomography.

Project description:IntroductionAlthough positron emission tomography/computed tomography (PET/CT) is a common tool for measuring breast cancer (BC), subtypes are not automatically classified by it. Therefore, the purpose of this research is to use an artificial neural network (ANN) to evaluate the clinical subtypes of BC based on the value of the tumor marker.Materials and methodsIn our nuclear medical facility, 122 BC patients (training and testing) had 18F-fluoro-D-glucose (18F-FDG) PET/CT to identify the various subtypes of the disease. 18F-FDG-18 injections were administered to the patients before the scanning process. We carried out the scan according to protocol. Based on the tumor marker value, the ANN's output layer uses the Softmax function with cross-entropy loss to detect different subtypes of BC.ResultsWith an accuracy of 95.77%, the result illustrates the ANN model for K-fold cross-validation. The mean values of specificity and sensitivity were 0.955 and 0.958, respectively. The area under the curve on average was 0.985.ConclusionSubtypes of BC may be categorized using the suggested approach. The PET/CT may be updated to diagnose BC subtypes using the appropriate tumor maker value when the suggested model is clinically implemented.

| S-EPMC11309150 | biostudies-literature