The Place of PET to Assess New Therapeutic Effectiveness in Neurodegenerative Diseases

Dupont, Anne-Claire; Largeau, Bérenger; Guilloteau, Denis; Ribeiro, Maria João; Arlicot, Nicolas

doi:10.1155/2018/7043578

Cited by 17 publications

(7 citation statements)

References 91 publications

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“…It also provided an insight into the pathophysiological pathway concerned with ND. Recently, the progression of PET radioligands subjected to accurate in vivo neuroimaging has been the main research attraction and due to PET, various pathophysiological processes associated with ND (neurotransmission, neuroinflammation and aggregation of protein) could be explored (Dupont et al, 2018). Terada et al, 2022 utilized PET with [ 18 F]2-tert-butyl-4chloro-5-2H-pyridazin-3-one (BCPP-EF) to measure mitochondrial complex I (site of ROS production) in patients with mild AD.…”

Section: Unmet Challenges and Future Prospects Positron Emission Tomo...mentioning

confidence: 99%

Resveratrol: A potential therapeutic natural polyphenol for neurodegenerative diseases associated with mitochondrial dysfunction

Yadav

Khan

et al. 2022

Front. Pharmacol.

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Most polyphenols can cross blood-brain barrier, therefore, they are widely utilized in the treatment of various neurodegenerative diseases (ND). Resveratrol, a natural polyphenol contained in blueberry, grapes, mulberry, etc., is well documented to exhibit potent neuroprotective activity against different ND by mitochondria modulation approach. Mitochondrial function impairment is the most common etiology and pathological process in various neurodegenerative disorders, viz. Alzheimer’s disease, Parkinson’s disease, Huntington’s disease and amyotrophic lateral sclerosis. Nowadays these ND associated with mitochondrial dysfunction have become a major threat to public health as well as health care systems in terms of financial burden. Currently available therapies for ND are limited to symptomatic cures and have inevitable toxic effects. Therefore, there is a strict requirement for a safe and highly effective drug treatment developed from natural compounds. The current review provides updated information about the potential of resveratrol to target mitochondria in the treatment of ND.

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Section: Unmet Challenges and Future Prospects Positron Emission Tomo...mentioning

confidence: 99%

Resveratrol: A potential therapeutic natural polyphenol for neurodegenerative diseases associated with mitochondrial dysfunction

Yadav

Khan

et al. 2022

Front. Pharmacol.

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“…These particular targets have multiple PET tracers, which are very necessary and possess superior properties for drug improvement, characterization, and to diagnose the inflammation sites. This review mainly described multiple tracers, synaptics, and targets, which have been injected into humans (Dupont et al, 2018; Imming et al, 2006). Few well‐known in‐human tracers belonging to different targets are given in Figure 4.…”

Section: Methodsmentioning

confidence: 99%

Evaluation of advanced, pathophysiologic new targets for imaging of CNS

Singh

Srivastava

et al. 2023

Drug Development Research

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The inadequate information about the in vivo pathological, physiological, and neurological impairments, as well as the absence of in vivo tools for assessing brain penetrance and the efficiency of newly designed drugs, has hampered the development of new techniques for the treatment for variety of new central nervous system (CNS) diseases. The searching sites such as Science Direct and PubMed were used to find out the numerous distinct tracers across 16 CNS targets including tau, synaptic vesicle glycoprotein, the adenosine 2A receptor, the phosphodiesterase enzyme PDE10A, and the purinoceptor, among others. Among the most encouraging are [ 18 F]FIMX for mGluR imaging, [ 11 C]Martinostat for Histone deacetylase, [ 18 F]MNI-444 for adenosine 2A imaging, [ 11 C]ER176 for translocator protein, and [ 18 F]MK-6240 for tau imaging. We also reviewed the findings for each tracer's features and potential for application in CNS pathophysiology and therapeutic evaluation investigations, including target specificity, binding efficacy, and pharmacokinetic factors. This review aims to present a current evaluation of modern positron emission tomography tracers for CNS targets, with a focus on recent advances for targets that have newly emerged for imaging in humans.

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“…Additionally, multiple targets within this section are linked to degenerative neurological disorders. PET tracers for these targets are therefore of great importance for characterisation of a wide range of diseases, diagnosis, and drug development programmes [173]. Table 3 highlights the recent tracers for receptor, transporter, and synaptic targets that have been translated into humans from 2013 to 2018.…”

Section: Receptor Transporter and Synaptic Targetsmentioning

confidence: 99%

Advances in CNS PET: the state-of-the-art for new imaging targets for pathophysiology and drug development

McCluskey

Plisson

Rabiner

et al. 2019

Eur J Nucl Med Mol Imaging

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Purpose A limit on developing new treatments for a number of central nervous system (CNS) disorders has been the inadequate understanding of the in vivo pathophysiology underlying neurological and psychiatric disorders and the lack of in vivo tools to determine brain penetrance, target engagement, and relevant molecular activity of novel drugs. Molecular neuroimaging provides the tools to address this. This article aims to provide a state-of-the-art review of new PET tracers for CNS targets, focusing on developments in the last 5 years for targets recently available for inhuman imaging. Methods We provide an overview of the criteria used to evaluate PET tracers. We then used the National Institute of Mental Health Research Priorities list to identify the key CNS targets. We conducted a PubMed search (search period 1st of January 2013 to 31st of December 2018), which yielded 40 new PET tracers across 16 CNS targets which met our selectivity criteria. For each tracer, we summarised the evidence of its properties and potential for use in studies of CNS pathophysiology and drug evaluation, including its target selectivity and affinity, inter and intra-subject variability, and pharmacokinetic parameters. We also consider its potential limitations and missing characterisation data, but not specific applications in drug development. Where multiple tracers were present for a target, we provide a comparison of their properties. Results and conclusions Our review shows that multiple new tracers have been developed for proteinopathy targets, particularly tau, as well as the purinoceptor P2X7, phosphodiesterase enzyme PDE10A, and synaptic vesicle glycoprotein 2A (SV2A), amongst others. Some of the most promising of these include 18 F-MK-6240 for tau imaging, 11 C-UCB-J for imaging SV2A, 11 C-CURB and 11 C-MK-3168 for characterisation of fatty acid amide hydrolase, 18 F-FIMX for metabotropic glutamate receptor 1, and 18 F-MNI-444 for imaging adenosine 2A. Our review also identifies recurrent issues within the field. Many of the tracers discussed lack in vivo blocking data, reducing confidence in selectivity. Additionally, late-stage identification of substantial off-target sites for multiple tracers highlights incomplete preclinical characterisation prior to translation, as well as human disease state studies carried out without confirmation of test-retest reproducibility.

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The Place of PET to Assess New Therapeutic Effectiveness in Neurodegenerative Diseases

Cited by 17 publications

References 91 publications

Resveratrol: A potential therapeutic natural polyphenol for neurodegenerative diseases associated with mitochondrial dysfunction

Resveratrol: A potential therapeutic natural polyphenol for neurodegenerative diseases associated with mitochondrial dysfunction

Evaluation of advanced, pathophysiologic new targets for imaging of CNS

Advances in CNS PET: the state-of-the-art for new imaging targets for pathophysiology and drug development

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