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Journal articles on the topic 'TSPO binding'

Author: Grafiati

Published: 2 June 2025

Last updated: 31 July 2025

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1

Iatmanen-Harbi, Soria, lucile Senicourt, Vassilios Papadopoulos, Olivier Lequin, and Jean-Jacques Lacapere. "Characterization of the High-Affinity Drug Ligand Binding Site of Mouse Recombinant TSPO." International Journal of Molecular Sciences 20, no. 6 (2019): 1444. http://dx.doi.org/10.3390/ijms20061444.

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The optimization of translocator protein (TSPO) ligands for Positron Emission Tomography as well as for the modulation of neurosteroids is a critical necessity for the development of TSPO-based diagnostics and therapeutics of neuropsychiatrics and neurodegenerative disorders. Structural hints on the interaction site and ligand binding mechanism are essential for the development of efficient TSPO ligands. Recently published atomic structures of recombinant mammalian and bacterial TSPO1, bound with either the high-affinity drug ligand PK 11195 or protoporphyrin IX, have revealed the membrane pro

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2

Tong, Junchao, Belinda Williams, Pablo M. Rusjan, et al. "Concentration, distribution, and influence of aging on the 18 kDa translocator protein in human brain: Implications for brain imaging studies." Journal of Cerebral Blood Flow & Metabolism 40, no. 5 (2019): 1061–76. http://dx.doi.org/10.1177/0271678x19858003.

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Positron emission tomography (PET) imaging of the translocator protein (TSPO) is widely used as a biomarker of microglial activation. However, TSPO protein concentration in human brain has not been optimally quantified nor has its regional distribution been compared to TSPO binding. We determined TSPO protein concentration, change with age, and regional distribution by quantitative immunoblotting in autopsied human brain. Brain TSPO protein concentration (>0.1 ng/µg protein) was higher than those reported by in vitro binding assays by at least 2 to 70 fold. TSPO protein distributed widely i

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3

Owen, David R., Astrid J. Yeo, Roger N. Gunn, et al. "An 18-kDa Translocator Protein (TSPO) Polymorphism Explains Differences in Binding Affinity of the PET Radioligand PBR28." Journal of Cerebral Blood Flow & Metabolism 32, no. 1 (2011): 1–5. http://dx.doi.org/10.1038/jcbfm.2011.147.

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[11C]PBR28 binds the 18-kDa Translocator Protein (TSPO) and is used in positron emission tomography (PET) to detect microglial activation. However, quantitative interpretations of signal are confounded by large interindividual variability in binding affinity, which displays a trimodal distribution compatible with a codominant genetic trait. Here, we tested directly for an underlying genetic mechanism to explain this. Binding affinity of PBR28 was measured in platelets isolated from 41 human subjects and tested for association with polymorphisms in TSPO and genes encoding other proteins in the

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Asih, Prita R., Anne Poljak, Michael Kassiou, Yazi D. Ke, and Lars M. Ittner. "Differential mitochondrial protein interaction profile between human translocator protein and its A147T polymorphism variant." PLOS ONE 17, no. 5 (2022): e0254296. http://dx.doi.org/10.1371/journal.pone.0254296.

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The translocator protein (TSPO) has been implicated in mitochondrial transmembrane cholesterol transport, brain inflammation, and other mitochondrial functions. It is upregulated in glial cells during neuroinflammation in Alzheimer’s disease. High affinity TSPO imaging radioligands are utilized to visualize neuroinflammation. However, this is hampered by the common A147T polymorphism which compromises ligand binding. Furthermore, this polymorphism has been linked to increased risk of neuropsychiatric disorders, and possibly reduces TSPO protein stability. Here, we used immunoprecipitation coup

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5

Berroterán-Infante, Neydher, Monika Tadić, Marcus Hacker, Wolfgang Wadsak, and Markus Mitterhauser. "Binding Affinity of Some Endogenous and Synthetic TSPO Ligands Regarding the rs6971 Polymorphism." International Journal of Molecular Sciences 20, no. 3 (2019): 563. http://dx.doi.org/10.3390/ijms20030563.

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An intriguing target involved in several pathophysiological processes is the 18 kDa translocator protein (TSPO), of which exact functions remained elusive until now. A single nucleotide polymorphism in the TSPO gene influences the binding affinity of endogenous and synthetic TSPO ligands by facilitating a lower-affinity conformation, which modifies a potential ligand binding site, ultimately leading to a binding profile classification according to each genotype. For instance, some clinical effects of the distinctive binding affinity profile of cholesterol toward the TSPO of individuals with di

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Kreisl, William C., Kimberly J. Jenko, Christina S. Hines, et al. "A Genetic Polymorphism for Translocator Protein 18 Kda Affects both in Vitro and in Vivo Radioligand Binding in Human Brain to this Putative Biomarker of Neuroinflammation." Journal of Cerebral Blood Flow & Metabolism 33, no. 1 (2012): 53–58. http://dx.doi.org/10.1038/jcbfm.2012.131.

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Second-generation radioligands for translocator protein (TSPO), an inflammation marker, are confounded by the codominant rs6971 polymorphism that affects binding affinity. The resulting three groups are homozygous for high-affinity state (HH), homozygous for low-affinity state (LL), or heterozygous (HL). We tested if in vitro binding to leukocytes distinguished TSPO genotypes and if genotype could affect clinical studies using the TSPO radioligand [11C]PBR28. In vitro binding to leukocytes and [11C]PBR28 brain imaging were performed in 27 human subjects with known TSPO genotype. Specific [3H]P

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7

Tournier, Benjamin B., Stergios Tsartsalis, Kelly Ceyzériat, et al. "Fluorescence-activated cell sorting to reveal the cell origin of radioligand binding." Journal of Cerebral Blood Flow & Metabolism 40, no. 6 (2019): 1242–55. http://dx.doi.org/10.1177/0271678x19860408.

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Many studies have explored the role of TSPO (18 kDa translocator protein) as a marker of neuroinflammation using single-photon emission computed tomography (SPECT) or positron emission tomography (PET). In vivo imaging does not allow to determine the cells in which TSPO is altered. We propose a methodology based on fluorescence-activated cell sorting to sort different cell types of radioligand-treated tissues. We compared left/right hippocampus of rats in response to a unilateral injection of lipopolysaccharide (LPS), ciliary neurotrophic factor (CNTF) or saline. We finally applied this method

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8

Hiser, Carrie, Beronda L. Montgomery, and Shelagh Ferguson-Miller. "TSPO protein binding partners in bacteria, animals, and plants." Journal of Bioenergetics and Biomembranes 53, no. 4 (2021): 463–87. http://dx.doi.org/10.1007/s10863-021-09905-4.

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AbstractThe ancient membrane protein TSPO is phylogenetically widespread from archaea and bacteria to insects, vertebrates, plants, and fungi. TSPO’s primary amino acid sequence is only modestly conserved between diverse species, although its five transmembrane helical structure appears mainly conserved. Its cellular location and orientation in membranes have been reported to vary between species and tissues, with implications for potential diverse binding partners and function. Most TSPO functions relate to stress-induced changes in metabolism, but in many cases it is unclear how TSPO itself

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Vo, Sophie V., Samuel D. Banister, Isaac Freelander, et al. "Reversing binding sensitivity to A147T translocator protein." RSC Medicinal Chemistry 11, no. 4 (2020): 511–17. http://dx.doi.org/10.1039/c9md00580c.

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10

Wimberley, Catriona, Sonia Lavisse, Vincent Brulon, et al. "Impact of Endothelial 18-kDa Translocator Protein on the Quantification of 18F-DPA-714." Journal of Nuclear Medecine 59, no. 2 (2017): 307–14. https://doi.org/10.2967/jnumed.117.195396.

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Abstract <sup>18</sup>F-DPA-714 is a second-generation tracer for PET imaging of the 18-kDa translocator protein (TSPO), a marker of neuroinflammation. Analysis and interpretation of TSPO PET are challenging, especially because of the basal expression of TSPO. The aim of this study was to evaluate a compartmental model that accounts for the effect of endothelial TSPO binding on the quantification of <sup>18</sup>F-DPA-714 PET scans from a cohort of healthy subjects. <strong>Methods:</strong> Fifteen healthy subjects (9 high-affinity binders and 6 mixed-affinity binders) underwent <sup>18</sup>

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Lee, Sang Hee, Nunzio Denora, Valentino Laquintana, et al. "Radiosynthesis and characterization of [18F]BS224: a next-generation TSPO PET ligand insensitive to the rs6971 polymorphism." European Journal of Nuclear Medicine and Molecular Imaging 49, no. 1 (2021): 110–24. http://dx.doi.org/10.1007/s00259-021-05617-4.

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Abstract Purpose Translocator protein 18-kDa (TSPO) positron emission tomography (PET) is a valuable tool to detect neuroinflammed areas in a broad spectrum of neurodegenerative diseases. However, the clinical application of second-generation TSPO ligands as biomarkers is limited because of the presence of human rs6971 polymorphism that affects their binding. Here, we describe the ability of a new TSPO ligand, [18F]BS224, to identify abnormal TSPO expression in neuroinflammation independent of the rs6971 polymorphism. Methods An in vitro competitive inhibition assay of BS224 was conducted with

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Werry, Eryn L., Fiona M. Bright, Olivier Piguet, et al. "Recent Developments in TSPO PET Imaging as A Biomarker of Neuroinflammation in Neurodegenerative Disorders." International Journal of Molecular Sciences 20, no. 13 (2019): 3161. http://dx.doi.org/10.3390/ijms20133161.

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Neuroinflammation is an inflammatory response in the brain and spinal cord, which can involve the activation of microglia and astrocytes. It is a common feature of many central nervous system disorders, including a range of neurodegenerative disorders. An overlap between activated microglia, pro-inflammatory cytokines and translocator protein (TSPO) ligand binding was shown in early animal studies of neurodegeneration. These findings have been translated in clinical studies, where increases in TSPO positron emission tomography (PET) signal occur in disease-relevant areas across a broad spectru

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13

Marques, Tiago Reis, Mattia Veronese, David R. Owen, Eugenii A. Rabiner, Graham E. Searle, and Oliver D. Howes. "Specific and non-specific binding of a tracer for the translocator-specific protein in schizophrenia: an [11C]-PBR28 blocking study." European Journal of Nuclear Medicine and Molecular Imaging 48, no. 11 (2021): 3530–39. http://dx.doi.org/10.1007/s00259-021-05327-x.

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Abstract Objective The mitochondrial 18-kDa translocator protein (TSPO) is expressed by activated microglia and positron emission tomography enables the measurement of TSPO levels in the brain. Findings in schizophrenia have shown to vary depending on the outcome measure used and this discrepancy in TSPO results could be explained by lower non-displaceable binding (VND) in schizophrenia, which could obscure increases in specific binding. In this study, we have used the TSPO ligand XBD173 to block the TSPO radioligand [11C]-PBR28 and used an occupancy plot to quantify VND in patients with schiz

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14

Tournier, Benjamin B., Stergios Tsartsalis, Kelly Ceyzériat, et al. "Astrocytic TSPO Upregulation Appears Before Microglial TSPO in Alzheimer’s Disease." Journal of Alzheimer's Disease 77, no. 3 (2020): 1043–56. http://dx.doi.org/10.3233/jad-200136.

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Background: In vivo PET/SPECT imaging of neuroinflammation is primarily based on the estimation of the 18 kDa-translocator-protein (TSPO). However, TSPO is expressed by different cell types which complicates the interpretation. Objective: The present study evaluates the cellular origin of TSPO alterations in Alzheimer’s disease (AD). Methods: The TSPO cell origin was evaluated by combining radioactive imaging approaches using the TSPO radiotracer [125I]CLINDE and fluorescence-activated cell sorting, in a rat model of AD (TgF344-AD) and in AD subjects. Results: In the hippocampus of TgF344-AD r

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Narlawar, Rajeshwar, Eryn L. Werry, Alana M. Scarf, et al. "First Demonstration of Positive Allosteric-like Modulation at the Human Wild Type Translocator Protein (TSPO)." J Med Chem. 58, no. 21 (2015): 8743–9. https://doi.org/10.1021/acs.jmedchem.5b01288.

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We show that changing the number and position of nitrogen atoms in the heteroatomic core of a pyrazolopyrimidine acetamide is sufficient to induce complex binding to wild type human TSPO. Only compounds with this complex binding profile lacked intrinsic effect on glioblastoma proliferation but positively modulated the antiproliferative effects of a synthetic TSPO ligand. To the best of our knowledge this is the first demonstration of allosteric-like interaction at the wild type human TSPO.

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Kanegawa, Naoki, Karin Collste, Anton Forsberg, et al. "In vivo evidence of a functional association between immune cells in blood and brain in healthy human subjects." Brain, Behavior and Immunity 54 (January 25, 2016): 149–57. https://doi.org/10.1016/j.bbi.2016.01.019.

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Microglia, the resident macrophages in the central nervous system, are thought to be maintained by a local self-renewal mechanism. Although preclinical and in vitro studies have suggested that the brain may contain immune cells also from peripheral origin, the functional association between immune cells in the periphery and brain at physiological conditions is poorly understood. We examined 32 healthy individuals using positron emission tomography (PET) and [<sup>11</sup>C]PBR28, a radioligand for the 18-kDa translocator protein (TSPO) which is expressed both in brain microglia and blood immun

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Owen, David R., Nehal Narayan, Lisa Wells, et al. "Pro-inflammatory activation of primary microglia and macrophages increases 18 kDa translocator protein expression in rodents but not humans." Journal of Cerebral Blood Flow & Metabolism 37, no. 8 (2017): 2679–90. http://dx.doi.org/10.1177/0271678x17710182.

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The 18kDa Translocator Protein (TSPO) is the most commonly used tissue-specific marker of inflammation in positron emission tomography (PET) studies. It is expressed in myeloid cells such as microglia and macrophages, and in rodent myeloid cells expression increases with cellular activation. We assessed the effect of myeloid cell activation on TSPO gene expression in both primary human and rodent microglia and macrophages in vitro, and also measured TSPO radioligand binding with 3H-PBR28 in primary human macrophages. As observed previously, we found that TSPO expression increases (∼9-fold) in

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Cumming, Paul, Bjorn Burgher, Omkar Patkar, et al. "Sifting through the surfeit of neuroinflammation tracers." Journal of Cerebral Blood Flow & Metabolism 38, no. 2 (2017): 204–24. http://dx.doi.org/10.1177/0271678x17748786.

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The first phase of molecular brain imaging of microglial activation in neuroinflammatory conditions began some 20 years ago with the introduction of [11C]-( R)-PK11195, the prototype isoquinoline ligand for translocator protein (18 kDa) (TSPO). Investigations by positron emission tomography (PET) revealed microgliosis in numerous brain diseases, despite the rather low specific binding signal imparted by [11C]-( R)-PK11195. There has since been enormous expansion of the repertoire of TSPO tracers, many with higher specific binding, albeit complicated by allelic dependence of the affinity. Howev

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Thejer, Bashar M., Vittoria Infantino, Anna Santarsiero, et al. "Sigma-2 Receptor Ligand Binding Modulates Association between TSPO and TMEM97." International Journal of Molecular Sciences 24, no. 7 (2023): 6381. http://dx.doi.org/10.3390/ijms24076381.

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Sigma-2 receptor (S2R) is a S2R ligand-binding site historically associated with reportedly 21.5 kDa proteins that have been linked to several diseases, such as cancer, Alzheimer’s disease, and schizophrenia. The S2R is highly expressed in various tumors, where it correlates with the proliferative status of the malignant cells. Recently, S2R was reported to be the transmembrane protein TMEM97. Prior to that, we had been investigating the translocator protein (TSPO) as a potential 21.5 kDa S2R candidate protein with reported heme and sterol associations. Here, we investigate the contributions o

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Owen, David R., Owain W. Howell, Sac-Pham Tang, et al. "Two Binding Sites for [3H]PBR28 in Human Brain: Implications for TSPO PET Imaging of Neuroinflammation." Journal of Cerebral Blood Flow & Metabolism 30, no. 9 (2010): 1608–18. http://dx.doi.org/10.1038/jcbfm.2010.63.

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[11C]PBR28, a radioligand targeting the translocator protein (TSPO), does not produce a specific binding signal in approximately 14% of healthy volunteers. This phenomenon has not been reported for [11C]PK11195, another TSPO radioligand. We measured the specific binding signals with [3H]PK11195 and [3H]PBR28 in brain tissue from 22 donors. Overall, 23% of the samples did not generate a visually detectable specific autoradiographic signal with [3H]PBR28, although all samples showed [3H]PK11195 binding. There was a marked reduction in the affinity of [3H]PBR28 for TSPO in samples with no visible

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Mizrahi, Romina, Pablo M. Rusjan, James Kennedy, et al. "Translocator Protein (18 kDa) Polymorphism (rs6971) Explains in-vivo Brain Binding Affinity of the PET Radioligand [18F]-FEPPA." Journal of Cerebral Blood Flow & Metabolism 32, no. 6 (2012): 968–72. http://dx.doi.org/10.1038/jcbfm.2012.46.

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[18F]-FEPPA binds to the 18-kDa translocator protein (TSPO) and is used in positron emission tomography (PET) to detect microglial activation. However, quantitative interpretations of the PET signal with new generation TSPO PET radioligands are confounded by large interindividual variability in binding affinity. This presents as a trimodal distribution, reflecting high-affinity binders (HABs), low-affinity binder (LAB), and mixed-affinity binders (MABs). Here, we show that one polymorphism (rs6971) located in exon 4 of the TSPO gene, which results in a nonconservative amino-acid substitution f

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Betlazar, Calina, Meredith Harrison-Brown, Ryan Middleton, Richard Banati, and Guo-Jun Liu. "Cellular Sources and Regional Variations in the Expression of the Neuroinflammatory Marker Translocator Protein (TSPO) in the Normal Brain." International Journal of Molecular Sciences 19, no. 9 (2018): 2707. http://dx.doi.org/10.3390/ijms19092707.

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The inducible expression of the mitochondrial translocator protein 18 kDa (TSPO) by activated microglia is a prominent, regular feature of acute and chronic-progressive brain pathology. This expression is also the rationale for the continual development of new TSPO binding molecules for the diagnosis of “neuroinflammation” by molecular imaging. However, there is in the normal brain an ill-defined, low-level constitutive expression of TSPO. Taking advantage of healthy TSPO knockout mouse brain tissue to validate TSPO antibody specificity, this study uses immunohistochemistry to determine the re

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van den Ameele, Jelle, Young T. Hong, Roido Manavaki, et al. "[11C]PK11195-PET Brain Imaging of the Mitochondrial Translocator Protein in Mitochondrial Disease." Neurology 96, no. 22 (2021): e2761-e2773. http://dx.doi.org/10.1212/wnl.0000000000012033.

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ObjectiveTo explore the possibilities of radioligands against the mitochondrial outer membrane translocator protein (TSPO) as biomarkers for mitochondrial disease, we performed brain PET-MRI with [11C]PK11195 in 14 patients with genetically confirmed mitochondrial disease and 33 matched controls.MethodsCase–control study of brain PET-MRI with the TSPO radioligand [11C]PK11195.ResultsForty-six percent of symptomatic patients had volumes of abnormal radiotracer binding greater than the 95th percentile in controls. [11C]PK11195 binding was generally greater in gray matter and significantly decrea

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Midzak, Andrew, Barry Zirkin, and Vassilios Papadopoulos. "Translocator protein: pharmacology and steroidogenesis." Biochemical Society Transactions 43, no. 4 (2015): 572–78. http://dx.doi.org/10.1042/bst20150061.

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The translocator protein (TSPO; 18k Da) is an evolutionarily conserved outer mitochondrial membrane (OMM) protein highly expressed in steroid-synthesizing cells and found to possess a number of physiological and drug-binding partners. Extensive pharmacological, biochemical and cell biological research over the years has led to a model of TSPO involvement in mitochondrial cholesterol transport and promotion of steroid synthesis, a model guiding the design of drugs useful in stimulating neurosteroid synthesis and alleviating psychopathological symptoms. The involvement of TSPO in these processes

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Su, Zhangjie, Federico Roncaroli, Pascal F. Durrenberger, et al. "The 18-kDa Mitochondrial Translocator Protein in Human Gliomas: A 11C-(R)PK11195 PET Imaging and Neuropathology Study." Journal of Nuclear Medicine 56, no. 4 (2015): 512–7. https://doi.org/10.2967/jnumed.114.151621.

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The 18-kDa mitochondrial translocator protein (TSPO) is up-regulated in high grade astrocytomas and can be imaged by positron emission tomography (PET) using the selective radiotracer 11C-(R)PK11195. We investigated 11C-(R)PK11195 binding in human gliomas and its relationship with TSPO expression in tumor tissue and glioma associated microglia/macrophages within the tumors. METHODS: Twenty-two glioma patients underwent dynamic 11C-(R)PK11195 PET scans and perfusion MRI acquisition. Parametric maps of 11C-(R)PK11195 binding potential (BPND) were generated. Co-registered

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Dickens, Alex M., Susanne Vainio, Päivi Marjamäki, et al. "Detection of Microglial Activation in an Acute Model of Neuroinflammation Using PET and Radiotracers 11C-(R)-PK11195 and 18F-GE-180." J Nucl Med. 55, no. 3 (2014): 466–72. https://doi.org/10.2967/jnumed.113.125625.

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It remains unclear how different translocator protein (TSPO) ligands reflect the spatial extent of astrocyte or microglial activation in various neuroinflammatory conditions. Here, we use a reproducible lipopolysaccharide (LPS)-induced model of acute central nervous system inflammation to compare the binding performance of a new TSPO ligand (18)F-GE-180 with (11)C-(R)-PK11195. Using immunohistochemistry, we also explore the ability of the TSPO ligands to detect activated microglial cells and astrocytes. METHODS: Lewis rats (n = 30) were microinjected with LPS (1 or 10 μg) or saline (1 μL

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Veronese, Mattia, Marcello Tuosto, Tiago Reis Marques, et al. "Parametric Mapping for TSPO PET Imaging with Spectral Analysis Impulsive Response Function." Molecular Imaging and Biology 23, no. 4 (2021): 560–71. http://dx.doi.org/10.1007/s11307-020-01575-9.

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Abstract Purpose The aim of this study was to investigate the use of spectral analysis (SA) for voxel-wise analysis of TSPO PET imaging studies. TSPO PET quantification is methodologically complicated by the heterogeneity of TSPO expression and its cell-dependent modulation during neuroinflammatory response. Compartmental models to account for this complexity exist, but they are unreliable at the high noise typical of voxel data. On the contrary, SA is noise-robust for parametric mapping and provides useful information about tracer kinetics with a free compartmental structure. Procedures SA im

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Gatliff, Jemma, and Michelangelo Campanella. "TSPO is a REDOX regulator of cell mitophagy." Biochemical Society Transactions 43, no. 4 (2015): 543–52. http://dx.doi.org/10.1042/bst20150037.

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The mitochondrial 18-kDa translocator protein (TSPO) was originally discovered as a peripheral binding site of benzodiazepines to be later described as a core element of cholesterol trafficking between cytosol and mitochondria from which the current nomenclature originated. The high affinity it exhibits with chemicals (i.e. PK11195) has generated interest in the development of mitochondrial based TSPO-binding drugs for in vitro and in vivo analysis. Increased TSPO expression is observed in numerous pathologies such as cancer and inflammatory conditions of the central nervous system (CNS) that

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Milenkovic, Vladimir M., Dounia Slim, Stefanie Bader, et al. "CRISPR-Cas9 Mediated TSPO Gene Knockout alters Respiration and Cellular Metabolism in Human Primary Microglia Cells." International Journal of Molecular Sciences 20, no. 13 (2019): 3359. http://dx.doi.org/10.3390/ijms20133359.

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The 18 kDa translocator protein (TSPO) is an evolutionary conserved cholesterol binding protein localized in the outer mitochondrial membrane. It has been implicated in the regulation of various cellular processes including oxidative stress, proliferation, apoptosis, and steroid hormone biosynthesis. Since the expression of TSPO in activated microglia is upregulated in various neuroinflammatory and neurodegenerative disorders, we set out to examine the role of TSPO in an immortalized human microglia C20 cell line. To this end, we performed a dual approach and used (i) lentiviral shRNA silencin

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Radford-Smith, Daniel E., Abi G. Yates, Tereza Kacerova, et al. "Integrating TSPO-PET imaging with metabolomics for enhanced prognostic accuracy in multiple sclerosis." BMJ Neurology Open 7, no. 1 (2025): e001026. https://doi.org/10.1136/bmjno-2025-001026.

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BackgroundPredicting disease progression in multiple sclerosis (MS) remains challenging. PET imaging with 18 kDa translocator protein (TSPO) radioligands can detect microglial and astrocyte activation beyond MRI-visible lesions, which has been shown to be highly predictive of disease progression. We previously demonstrated that nuclear magnetic resonance (NMR)-based metabolomics could accurately distinguish between relapsing-remitting (RRMS) and secondary progressive MS (SPMS). This study investigates whether combining TSPO imaging with metabolomics enhances predictive accuracy in a similar se

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Rizzo, Gaia, Mattia Veronese, Matteo Tonietto, et al. "Generalization of endothelial modelling of TSPO PET imaging: Considerations on tracer affinities." Journal of Cerebral Blood Flow & Metabolism 39, no. 5 (2017): 874–85. http://dx.doi.org/10.1177/0271678x17742004.

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The 18 kDa translocator protein (TSPO) is a marker of microglia activation and the main target of positron emission tomography (PET) ligands for neuroinflammation. Previous works showed that accounting for TSPO endothelial binding improves PET quantification for [11C]PBR28, [18F]DPA714 and [11C]-R-PK11195. It is still unclear, however, whether the vascular signal is tracer-dependent. This work aims to explore the relationship between the TSPO vascular and tissue components for PET tracers with varying affinity, also assessing the impact of affinity towards the differentiability amongst kinetic

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Banister, Samuel D., Corinne Beinat, Shane M. Wilkinson, et al. "Ether analogues of DPA-714 with subnanomolar affinity for the translocator protein (TSPO)." Eur J Med Chem. 93 (February 7, 2015): 392–400. https://doi.org/10.1016/j.ejmech.2015.02.004.

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Sixteen new phenyl alkyl ether derivatives (12, 14-28) of the 5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-ylacetamide (DPA) class were synthesized and evaluated in a competition binding assay against [3H]PK11195 using 18 kDa translocator protein (TSPO) derived from rat kidney mitochondrial fractions. All analogues showed superior binding affinities for TSPO compared to DPA-713 (5) and DPA-714 (6). Picomolar affinities were observed for this class of TSPO ligands in this assay for the first time, with phenethyl ether 28 showing the greatest affinity (Ki = 0.13 nM). Additiona

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Hinz, Rainer, and Ronald Boellaard. "Challenges of quantification of TSPO in the human brain." Clinical and Translational Imaging 3, no. 6 (2015): 403–16. https://doi.org/10.1007/s40336-015-0138-7.

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The first positron emission tomography (PET) imaging studies in humans of the translocator protein 18kDa (TSPO) were conducted in the 1980ies with a primary interest in quantifying the binding in peripheral organs such as the heart, spleen and kidneys to what was then known as the peripheral benzodiazepine receptor.  However, the number of studies rapidly increased when the focus of the research shifted to the brain, and [<sup>11</sup>C](<em>R</em>)-PK11195 became <em>de facto</em> the reference radiotracer for all <em>in vivo</em> TSPO binding assays. For the quantitative analysis of the

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Vicidomini, Caterina, Mariarosaria Panico, Adelaide Greco, et al. "In vivo imaging and characterization of [(18)F]DPA-714, a potential new TSPO ligand, in mouse brain and peripheral tissues using small-animal PET." Nucl Med Biol. 42, no. 3 (2014): 309–16. https://doi.org/10.1016/j.nucmedbio.2014.11.009.

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INTRODUCTION: The translocator protein 18kDa (TSPO), a biochemical marker of neuroinflammation, is highly expressed in the brain activated microglia and it is also expressed by peripheral inflammatory cells and normal peripheral tissues. Thus, development of radioligands for the TSPO may contribute to further understanding the in vivo TSPO function in central and peripheral inflammatory processes and other pathologies. Here, we report the biodistribution, the specific binding and the radiometabolites of [(18)F]DPA-714, a promising fluorinated PET radiotracer, in normal mice using a microP

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Favreau, Frederic, Ludivine Rossard, Keqiang Zhang, et al. "Expression and modulation of translocator protein and its partners by hypoxia reoxygenation or ischemia and reperfusion in porcine renal models." American Journal of Physiology-Renal Physiology 297, no. 1 (2009): F177—F190. http://dx.doi.org/10.1152/ajprenal.90422.2008.

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Translocator protein (TSPO), formerly known as the peripheral-type benzodiazepine receptor, is an 18-kDa drug- and cholesterol-binding protein localized to the outer mitochondrial membrane and implicated in a variety of cell and mitochondrial functions. To determine the role of TSPO in ischemia-reperfusion injury (IRI), we used both in vivo and in vitro porcine models: an in vivo renal ischemia model where different conservation modalities were tested and an in vitro model where TSPO-transfected porcine proximal tubule LLC-PK1cells were exposed to hypoxia and oxidative stress. The expression o

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Plavén-Sigray, Pontus, Granville Matheson, Jennifer Coughlin, et al. "T7. UPDATED INDIVIDUAL PARTICIPANT DATA META-ANALYSIS CONFIRMS LOWER LEVELS OF THE GLIAL MARKER TSPO IN PSYCHOSIS PATIENTS." Schizophrenia Bulletin 46, Supplement_1 (2020): S233. http://dx.doi.org/10.1093/schbul/sbaa029.567.

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Abstract Background Treatment targeting the immune system is a promising new approach in schizophrenia. In search for tools for stratification and treatment monitoring, much effort has been invested in the use of positron emission tomography (PET) and radioligands binding to a glial marker, the 18 kDa translocator protein (TSPO). We previously demonstrated lower TSPO in psychosis patients in an individual participant data (IPD) meta-analysis of studies using second generation TSPO radioligands (Plavén-Sigray et al., 2018). Subsequently, a summary-statistics meta-analysis, including one newly p

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Donat, Cornelius K., Khaled Gaber, Jürgen Meixensberger, et al. "Changes in Binding of [123I]CLINDE, a High-Affinity Translocator Protein 18 kDa (TSPO) Selective Radioligand in a Rat Model of Traumatic Brain Injury." Neuromolecular Medecine 18, no. 2 (2016): 158–69. https://doi.org/10.1007/s12017-016-8385-y.

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After traumatic brain injury (TBI), secondary injuries develop, including neuroinflammatory processes that contribute to long-lasting impairments. These secondary injuries represent potential targets for treatment and diagnostics. The translocator protein 18 kDa (TSPO) is expressed in activated microglia cells and upregulated in response to brain injury and therefore a potential biomarker of the neuroinflammatory processes. Second-generation radioligands of TSPO, such as [<sup>123</sup>I]CLINDE, have a higher signal-to-noise ratio as the prototype ligand PK11195. [<sup>123</sup>I]CLINDE h

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Owen, David R., Qi Guo, Nicola J. Kalk, et al. "Determination of [11C]PBR28 Binding Potential in vivo: A First Human TSPO Blocking Study." Journal of Cerebral Blood Flow & Metabolism 34, no. 6 (2014): 989–94. http://dx.doi.org/10.1038/jcbfm.2014.46.

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Positron emission tomography (PET) targeting the 18 kDa translocator protein (TSPO) is used to quantify neuroinflammation. Translocator protein is expressed throughout the brain, and therefore a classical reference region approach cannot be used to estimate binding potential ( BP ND). Here, we used blockade of the TSPO radioligand [11C]PBR28 with the TSPO ligand XBD173, to determine the non-displaceable volume of distribution ( V ND), and hence estimate the BP ND. A total of 26 healthy volunteers, 16 high-affinity binders (HABs) and 10 mixed affinity binders (MABs) underwent a [11C]PBR28 PET s

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Feng, Ling, Claus Svarer, Gerda Thomsen, et al. "In vivo quantification of cerebral translocator protein binding in humans using 6-chloro-2-(4'-123I-iodophenyl)-3-(N,N-diethyl)-imidazo[1,2-a]pyridine-3-acetamide SPECT." J Nucl Med. 55, no. 12 (2014): 1966–72. https://doi.org/10.2967/jnumed.114.143727.

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This study provides the first comprehensive quantification of translocator protein (TSPO) binding using SPECT and 6-chloro-2-(4'-(123)I-iodophenyl)-3-(N,N-diethyl)-imidazo[1,2-a]pyridine-3-acetamide ((123)I-CLINDE) in neurologic patients. (123)I-CLINDE is structurally related to well-known PET ligands such as (18)F-PBR111 and (18)F-DPA-714. METHODS: Six patients with cerebral stroke and 4 patients with glioblastoma multiforme (GBM) underwent 150-min dynamic SPECT scans with arterial blood sampling. Four of the patients were rescanned. All patients were genotyped for the rs6971 polymor

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Veronese, Mattia, Tiago Reis Marques, Peter S. Bloomfield, et al. "Kinetic modelling of [11C]PBR28 for 18 kDa translocator protein PET data: A validation study of vascular modelling in the brain using XBD173 and tissue analysis." Journal of Cerebral Blood Flow & Metabolism 38, no. 7 (2017): 1227–42. http://dx.doi.org/10.1177/0271678x17712388.

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The 18 kDa translocator protein (TSPO) is a marker of microglia activation in the central nervous system and represents the main target of radiotracers for the in vivo quantification of neuroinflammation with positron emission tomography (PET). TSPO PET is methodologically challenging given the heterogeneous distribution of TSPO in blood and brain. Our previous studies with the TSPO tracers [11C]PBR28 and [11C]PK11195 demonstrated that a model accounting for TSPO binding to the endothelium improves the quantification of PET data. Here, we performed a validation of the kinetic model with the ad

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Fan, Jinjiang, Kevin Wang, Barry Zirkin, and Vassilios Papadopoulos. "CRISPR/Cas9‒Mediated Tspo Gene Mutations Lead to Reduced Mitochondrial Membrane Potential and Steroid Formation in MA-10 Mouse Tumor Leydig Cells." Endocrinology 159, no. 2 (2017): 1130–46. http://dx.doi.org/10.1210/en.2017-03065.

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Abstract The outer mitochondrial membrane translocator protein (TSPO) binds cholesterol with high affinity and is involved in mediating its delivery into mitochondria, the rate-limiting step in hormone-induced steroidogenesis. Specific ligand binding to TSPO has been shown to initiate steroid formation. However, recent studies of the genetic deletion of Tspo have provided conflicting results. Here, we address and extend previous studies by examining the effects of Tspo-specific mutations on steroid formation in hormone- and cyclic adenosine monophosphate (cAMP)–responsive MA-10 cells, using th

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Owen, David R., Jinjiang Fan, Enrico Campioli, et al. "TSPO mutations in rats and a human polymorphism impair the rate of steroid synthesis." Biochemical Journal 474, no. 23 (2017): 3985–99. http://dx.doi.org/10.1042/bcj20170648.

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The 18 kDa translocator protein (TSPO) is a ubiquitous conserved outer mitochondrial membrane protein implicated in numerous cell and tissue functions, including steroid hormone biosynthesis, respiration, cell proliferation, and apoptosis. TSPO binds with high affinity to cholesterol and numerous compounds, is expressed at high levels in steroid-synthesizing tissues, and mediates cholesterol import into mitochondria, which is the rate-limiting step in steroid formation. In humans, the rs6971 polymorphism on the TSPO gene leads to an amino acid substitution in the fifth transmembrane loop of th

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Farde, Lars. "TSPO binding may also represent ‘resting’ microglia." Clinical and Translational Imaging 3, no. 6 (2015): 491–92. http://dx.doi.org/10.1007/s40336-015-0155-6.

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Farde, Lars. "TSPO binding may also represent ‘resting’ microglia." Clinical and Translational Imaging 3, no. 6 (2015): 491–92. https://doi.org/10.1007/s40336-015-0155-6.

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Martín, Abraham, Raphaël Boisgard, Benoit Thézé, et al. "Evaluation of the PBR/TSPO Radioligand [18F]DPA-714 in a Rat Model of Focal Cerebral Ischemia." Journal of Cerebral Blood Flow & Metabolism 30, no. 1 (2009): 230–41. http://dx.doi.org/10.1038/jcbfm.2009.205.

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Focal cerebral ischemia leads to an inflammatory reaction involving an overexpression of the peripheral benzodiazepine receptor (PBR)/18-kDa translocator protein (TSPO) in the cerebral monocytic lineage (microglia and monocyte) and in astrocytes. Imaging of PBR/TSPO by positron emission tomography (PET) using radiolabeled ligands can document inflammatory processes induced by cerebral ischemia. We performed in vivo PET imaging with [18F]DPA-714 to determine the time course of PBR/TSPO expression over several days after induction of cerebral ischemia in rats. In vivo PET imaging showed signific

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Nack, Anne, Matthias Brendel, Julia Nedelcu, et al. "Expression of Translocator Protein and [18F]-GE180 Ligand Uptake in Multiple Sclerosis Animal Models." Cells 8, no. 2 (2019): 94. http://dx.doi.org/10.3390/cells8020094.

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Positron emission tomography (PET) ligands targeting the translocator protein (TSPO) represent promising tools to visualize neuroinflammation in multiple sclerosis (MS). Although it is known that TSPO is expressed in the outer mitochondria membrane, its cellular localization in the central nervous system under physiological and pathological conditions is not entirely clear. The purpose of this study was to assess the feasibility of utilizing PET imaging with the TSPO tracer, [18F]-GE180, to detect histopathological changes during experimental demyelination, and to determine which cell types ex

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Dimitrova-Shumkovska, Jasmina, Leo Veenman, Trpe Ristoski, Svetlana Leschiner, and Moshe Gavish. "Decreases in Binding Capacity of the Mitochondrial 18 kDa Translocator Protein Accompany Oxidative Stress and Pathological Signs in Rat Liver After DMBA Exposure." Toxicologic Pathology 38, no. 6 (2010): 957–68. http://dx.doi.org/10.1177/0192623310379137.

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7,12-Dimethylbenz[ a]anthracene (DMBA) presents a pollutant implicated in various toxicological effects. The aim of this experiment was to study the effects of DMBA administration on oxidative stress, histopathological signs, and 18 kDa translocator protein (TSPO) binding characteristics in rat liver. We also studied the effects of dose stoichiometry, dose frequency, and duration of protocol of DMBA administration. In this study, rats surviving eighteen weeks after DMBA exposure showed mild to moderate histopathological changes in the liver, mainly characterized by glossy appearance of hepatoc

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Selvaraj, Vimal, and Lan N. Tu. "Current status and future perspectives: TSPO in steroid neuroendocrinology." Journal of Endocrinology 231, no. 1 (2016): R1—R30. http://dx.doi.org/10.1530/joe-16-0241.

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The mitochondrial translocator protein (TSPO), previously known as the peripheral benzodiazepine receptor (PBR), has received significant attention both as a diagnostic biomarker and as a therapeutic target for different neuronal disease pathologies. Recently, its functional basis believed to be mediating mitochondrial cholesterol import for steroid hormone production has been refuted by studies examining both in vivo and in vitro genetic Tspo-deficient models. As a result, there now exists a fundamental gap in the understanding of TSPO function in the nervous system, and its putative pharmaco

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Georges, Elias, Chantal Sottas, Yuchang Li, and Vassilios Papadopoulos. "Direct and specific binding of cholesterol to the mitochondrial translocator protein (TSPO) using PhotoClick cholesterol analogue." Journal of Biochemistry, April 12, 2021. http://dx.doi.org/10.1093/jb/mvab031.

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Abstract The translocator protein (TSPO) is a five-helix transmembrane protein localized to the outer mitochondria membrane. Radioligand binding assays and chemical crosslinking showed TSPO to be a high affinity cholesterol-binding protein. In this report, we show that TSPO in mitochondrial fractions from MA-10 mouse tumour Leydig cells can interact directly and competitively with the clickable photoreactive cholesterol analogue. PhotoClick cholesterol showed saturable photoaffinity labelling of TSPO that could be specifically immunoprecipitated with anti-TSPO antibody, following the click rea

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Nutma, Erik, Kelly Ceyzériat, Sandra Amor, et al. "Cellular sources of TSPO expression in healthy and diseased brain." European Journal of Nuclear Medicine and Molecular Imaging, January 12, 2021. http://dx.doi.org/10.1007/s00259-020-05166-2.

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AbstractThe 18 kDa translocator protein (TSPO) is a highly conserved protein located in the outer mitochondrial membrane. TSPO binding, as measured with positron emission tomography (PET), is considered an in vivo marker of neuroinflammation. Indeed, TSPO expression is altered in neurodegenerative, neuroinflammatory, and neuropsychiatric diseases. In PET studies, the TSPO signal is often viewed as a marker of microglial cell activity. However, there is little evidence in support of a microglia-specific TSPO expression. This review describes the cellular sources and functions of TSPO in animal

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