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  • Article
  • Open Access
50 Citations
8,456 Views
35 Pages

Classical and Novel TSPO Ligands for the Mitochondrial TSPO Can Modulate Nuclear Gene Expression: Implications for Mitochondrial Retrograde Signaling

  • Nasra Yasin,
  • Leo Veenman,
  • Sukhdev Singh,
  • Maya Azrad,
  • Julia Bode,
  • Alex Vainshtein,
  • Beatriz Caballero,
  • Ilan Marek and
  • Moshe Gavish

It is known that knockdown of the mitochondrial 18 kDa translocator protein (TSPO) as well as TSPO ligands modulate various functions, including functions related to cancer. To study the ability of TSPO to regulate gene expression regarding such func...

  • Review
  • Open Access
23 Citations
5,881 Views
35 Pages

Translocator protein 18 kDa (TSPO) is a transmembrane protein in the mitochondrial membrane, which has been identified as a peripheral benzodiazepine receptor. TSPO is generally present at high concentrations in steroid-producing cells and plays an i...

  • Review
  • Open Access
41 Citations
9,642 Views
26 Pages

The 18 kDa translocator protein (TSPO) is highly 0conserved in eukaryotes and prokaryotes. Since its discovery in 1977, numerous studies established the TSPO’s importance for life essential functions. For these studies, synthetic TSPO ligands typical...

  • Review
  • Open Access
55 Citations
7,998 Views
26 Pages

The Role of Translocator Protein TSPO in Hallmarks of Glioblastoma

  • Laura-Marie Ammer,
  • Arabel Vollmann-Zwerenz,
  • Viktoria Ruf,
  • Christian H. Wetzel,
  • Markus J. Riemenschneider,
  • Nathalie L. Albert,
  • Philipp Beckhove and
  • Peter Hau

14 October 2020

Glioblastoma (GBM) is the most fatal primary brain cancer in adults. Despite extensive treatment, tumors inevitably recur, leading to an average survival time shorter than 1.5 years. The 18 kDa translocator protein (TSPO) is abundantly expressed thro...

  • Review
  • Open Access
78 Citations
8,225 Views
13 Pages

TSPO: An Evolutionarily Conserved Protein with Elusive Functions

  • Frederick Bonsack and
  • Sangeetha Sukumari-Ramesh

TSPO (18 kDa translocator protein) was identified decades ago in a search for peripheral tissue binding sites for benzodiazepines, and was formerly called the peripheral benzodiazepine receptor. TSPO is a conserved protein throughout evolution and it...

  • Article
  • Open Access
17 Citations
4,837 Views
14 Pages

Effects of Cigarette Smoke on TSPO-related Mitochondrial Processes

  • Nidal Zeineh,
  • Rafael Nagler,
  • Martin Gabay,
  • Abraham Weizman and
  • Moshe Gavish

10 July 2019

The 18 kDa translocator protein (TSPO) is an initiator of the mitochondrial apoptosis cascade. Cigarette smoke (CS) exposure provokes alterations in TSPO expression as well as upregulation of its related functions such as mitochondrial membrane poten...

  • Editorial
  • Open Access
29 Citations
4,983 Views
5 Pages

An Updated View of Translocator Protein (TSPO)

  • Nunzio Denora and
  • Giovanni Natile

6 December 2017

Decades of study on the role of mitochondria in living cells have evidenced the importance of the 18 kDa mitochondrial translocator protein (TSPO), first discovered in the 1977 as an alternative binding site for the benzodiazepine diazepam in the kid...

  • Review
  • Open Access
67 Citations
8,646 Views
34 Pages

In Vivo TSPO Signal and Neuroinflammation in Alzheimer’s Disease

  • Benjamin B. Tournier,
  • Stergios Tsartsalis,
  • Kelly Ceyzériat,
  • Valentina Garibotto and
  • Philippe Millet

21 August 2020

In the last decade, positron emission tomography (PET) and single-photon emission computed tomography (SPECT) in in vivo imaging has attempted to demonstrate the presence of neuroinflammatory reactions by measuring the 18 kDa translocator protein (TS...

  • Article
  • Open Access
63 Citations
6,833 Views
23 Pages

Translocator Protein (TSPO) as a Potential Biomarker in Human Cancers

  • Nimisha H. Bhoola,
  • Zukile Mbita,
  • Rodney Hull and
  • Zodwa Dlamini

TSPO is a receptor involved in the regulation of cellular proliferation, apoptosis and mitochondrial functions. Previous studies showed that the expression of TSPO protein correlated positively with tumour malignancy and negatively with patient survi...

  • Feature Paper
  • Article
  • Open Access
19 Citations
3,932 Views
15 Pages

Deletion of TSPO Causes Dysregulation of Cholesterol Metabolism in Mouse Retina

  • Fahad Farhan,
  • Mohammad Almarhoun,
  • Aileen Wong,
  • Amy S. Findlay,
  • Chris Bartholomew,
  • Mark T. S. Williams,
  • Toby W. Hurd and
  • Xinhua Shu

7 November 2021

Cholesterol dysregulation has been implicated in age-related macular degeneration (AMD), the most common cause of visual impairment in the elderly. The 18 KDa translocator protein (TSPO) is a mitochondrial outer membrane protein responsible for trans...

  • Article
  • Open Access
9 Citations
7,557 Views
13 Pages

TSPO Ligand-Methotrexate Prodrug Conjugates: Design, Synthesis, and Biological Evaluation

  • Valentino Laquintana,
  • Nunzio Denora,
  • Annalisa Cutrignelli,
  • Mara Perrone,
  • Rosa Maria Iacobazzi,
  • Cosimo Annese,
  • Antonio Lopalco,
  • Angela Assunta Lopedota and
  • Massimo Franco

The 18-kDa translocator protein (TSPO) is a potential mitochondrial target for drug delivery to tumors overexpressing TSPO, including brain cancers, and selective TSPO ligands have been successfully used to selectively deliver drugs into the target....

  • Review
  • Open Access
94 Citations
10,720 Views
17 Pages

The translocator protein (TSPO), located at the outer mitochondrial membrane (OMM), serves multiple functions and contributes to numerous processes, including cholesterol import, mitochondrial metabolism, apoptosis, cell proliferation, Ca2+ signaling...

  • Article
  • Open Access
18 Citations
4,628 Views
15 Pages

TSPO Deficiency Exacerbates GSDMD-Mediated Macrophage Pyroptosis in Inflammatory Bowel Disease

  • Xue Zhang,
  • Jingyi Han,
  • Yi Xu,
  • Menghua Cai,
  • Fei Gao,
  • Jiajia Han,
  • Dongdong Wang,
  • Yi Fu,
  • Hui Chen and
  • Jianmin Zhang
  • + 1 author

2 March 2022

Background: the 18-kDa translocator protein (TSPO) is a mitochondrial outer membrane protein, and its expression tends to increase in response to inflammatory stimulation, rapidly. However, the role of TSPO in inflammation and pyroptosis is not yet c...

  • Article
  • Open Access
23 Citations
4,889 Views
22 Pages

Delivery of Proapoptotic Agents in Glioma Cell Lines by TSPO Ligand–Dextran Nanogels

  • Antonio Lopalco,
  • Annalisa Cutrignelli,
  • Nunzio Denora,
  • Mara Perrone,
  • Rosa Maria Iacobazzi,
  • Elisabetta Fanizza,
  • Angela Lopedota,
  • Nicoletta Depalo,
  • Modesto De Candia and
  • Valentino Laquintana
  • + 1 author

Translocator protein 18-kDa (TSPO) is a versatile mitochondrial target for molecular imaging and therapy. Moreover, selective TSPO ligands have been widely investigated for diagnostic purposes and explored to target drug delivery systems directed to...

  • Article
  • Open Access
13 Citations
3,449 Views
20 Pages

The Comprehensive Steroidome in Complete TSPO/PBR Knockout Mice under Basal Conditions

  • Philippe Liere,
  • Guo-Jun Liu,
  • Antoine Pianos,
  • Ryan J. Middleton,
  • Richard B. Banati and
  • Yvette Akwa

27 January 2023

The 18 kDa translocator protein (TSPO/PBR) is a multifunctional evolutionary highly conserved outer mitochondrial membrane protein. Decades of research has reported an obligatory role of TSPO/PBR in both mitochondrial cholesterol transport and, thus,...

  • Article
  • Open Access
10 Citations
5,179 Views
20 Pages

Sigma-2 Receptor Ligand Binding Modulates Association between TSPO and TMEM97

  • Bashar M. Thejer,
  • Vittoria Infantino,
  • Anna Santarsiero,
  • Ilaria Pappalardo,
  • Francesca S. Abatematteo,
  • Sarah Teakel,
  • Ashleigh Van Oosterum,
  • Robert H. Mach,
  • Nunzio Denora and
  • Michael A. Cahill
  • + 8 authors

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 vari...

  • Communication
  • Open Access
18 Citations
4,788 Views
6 Pages

Binding Affinity of Some Endogenous and Synthetic TSPO Ligands Regarding the rs6971 Polymorphism

  • Neydher Berroterán-Infante,
  • Monika Tadić,
  • Marcus Hacker,
  • Wolfgang Wadsak and
  • Markus Mitterhauser

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...

  • Article
  • Open Access
13 Citations
5,089 Views
18 Pages

Characterization of the High-Affinity Drug Ligand Binding Site of Mouse Recombinant TSPO

  • Soria Iatmanen-Harbi,
  • lucile Senicourt,
  • Vassilios Papadopoulos,
  • Olivier Lequin and
  • Jean-Jacques Lacapere

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 ne...

  • Article
  • Open Access
17 Citations
4,288 Views
17 Pages

Deletion of TSPO Resulted in Change of Metabolomic Profile in Retinal Pigment Epithelial Cells

  • Abdulwahab Alamri,
  • Lincoln Biswas,
  • David G. Watson and
  • Xinhua Shu

Age-related macular degeneration is the main cause of vision loss in the aged population worldwide. Drusen, extracellular lesions formed underneath the retinal pigment epithelial (RPE) cells, are a clinical feature of AMD and associated with AMD prog...

  • Article
  • Open Access
21 Citations
4,572 Views
15 Pages

Downregulation of Mitochondrial TSPO Inhibits Mitophagy and Reduces Enucleation During Human Terminal Erythropoiesis

  • Martina Moras,
  • Claude Hattab,
  • Pedro Gonzalez-Menendez,
  • Suella Martino,
  • Jerome Larghero,
  • Caroline Le Van Kim,
  • Sandrina Kinet,
  • Naomi Taylor,
  • Sophie D. Lefevre and
  • Mariano A. Ostuni

28 November 2020

Translocator protein (TSPO) and voltage dependent anion channels (VDAC) are two proteins forming a macromolecular complex in the outer mitochondrial membrane that is involved in pleiotropic functions. Specifically, these proteins were described to re...

  • Article
  • Open Access
9 Citations
4,349 Views
16 Pages

Induction of ATP Release, PPIX Transport, and Cholesterol Uptake by Human Red Blood Cells Using a New Family of TSPO Ligands

  • Irene Marginedas-Freixa,
  • Cora L. Alvarez,
  • Martina Moras,
  • Claude Hattab,
  • Guillaume Bouyer,
  • Arnaud Chene,
  • Sophie D. Lefevre,
  • Caroline Le Van Kim,
  • Frederic Bihel and
  • Mariano A. Ostuni
  • + 1 author

10 October 2018

Two main isoforms of the Translocator Protein (TSPO) have been identified. TSPO1 is ubiquitous and is mainly present at the outer mitochondrial membrane of most eukaryotic cells, whereas, TSPO2 is specific to the erythroid lineage, located at the pla...

  • Article
  • Open Access
34 Citations
5,646 Views
17 Pages

Glioblastoma Exhibits Inter-Individual Heterogeneity of TSPO and LAT1 Expression in Neoplastic and Parenchymal Cells

  • Linzhi Cai,
  • Sabrina V. Kirchleitner,
  • Dongxu Zhao,
  • Min Li,
  • Jörg-Christian Tonn,
  • Rainer Glass and
  • Roland E. Kälin

Molecular imaging is essential for diagnosis and treatment planning for glioblastoma patients. Positron emission tomography (PET) with tracers for the detection of the solute carrier family 7 member 5 (SLC7A5; also known as the amino acid transporter...

  • Systematic Review
  • Open Access
11 Citations
3,367 Views
13 Pages

Clinical Applications of TSPO PET for Glioma Imaging: Current Evidence and Future Perspective—A Systematic Review

  • Luca Filippi,
  • Viviana Frantellizzi,
  • Giuseppe De Vincentis,
  • Orazio Schillaci and
  • Laura Evangelista

Our aim was to provide a comprehensive overview of the existing literature concerning the clinical applications of positron emission computed tomography (PET) with radiopharmaceuticals targeting the translocator protein (TSPO) in gliomas. A literatur...

  • Review
  • Open Access
14 Citations
4,769 Views
33 Pages

Radiotracers for Imaging of Inflammatory Biomarkers TSPO and COX-2 in the Brain and in the Periphery

  • Bright Chukwunwike Uzuegbunam,
  • Christoph Rummel,
  • Damiano Librizzi,
  • Carsten Culmsee and
  • Behrooz Hooshyar Yousefi

13 December 2023

Inflammation involves the activation of innate immune cells and is believed to play an important role in the development and progression of both infectious and non-infectious diseases such as neurodegeneration, autoimmune diseases, pulmonary and canc...

  • Article
  • Open Access
9 Citations
6,335 Views
15 Pages

6 September 2016

Translocator protein 18 kDa (TSPO) is a high affinity cholesterol- and drug-binding protein highly expressed in steroidogenic cells, such as Leydig cells, where it plays a role in cholesterol mitochondrial transport. We have previously shown that TSP...

  • Article
  • Open Access
8 Citations
6,503 Views
17 Pages

The Translocator Protein (TSPO) Genetic Polymorphism A147T Is Associated with Worse Survival in Male Glioblastoma Patients

  • Katie M. Troike,
  • Arlet M. Acanda de la Rocha,
  • Tyler J. Alban,
  • Matthew M. Grabowski,
  • Balint Otvos,
  • Gino Cioffi,
  • Kristin A. Waite,
  • Jill S. Barnholtz Sloan,
  • Justin D. Lathia and
  • Diana J. Azzam
  • + 1 author

8 September 2021

Glioblastoma (GBM) is the most common primary brain tumor in adults, with few available therapies and a five-year survival rate of 7.2%. Hence, strategies for improving GBM prognosis are urgently needed. The translocator protein 18kDa (TSPO) plays cr...

  • Article
  • Open Access
18 Citations
4,526 Views
16 Pages

Green Fluorescent Terbium (III) Complex Doped Silica Nanoparticles for TSPO Targeting

  • Elisabetta Fanizza,
  • Nicoletta Depalo,
  • Svetlana Fedorenko,
  • Rosa Maria Iacobazzi,
  • Alsu Mukhametshina,
  • Rustem Zairov,
  • Anastasio Salatino,
  • Fabio Vischio,
  • Annamaria Panniello and
  • Marinella Striccoli
  • + 4 authors

The low photostability of conventional organic dyes and the toxicity of cadmium-based luminescent quantum dots have prompted the development of novel probes for in vitro and in vivo labelling. Here, a new fluorescent lanthanide probe based on silica...

  • Article
  • Open Access
12 Citations
3,672 Views
20 Pages

The New Dipeptide TSPO Ligands: Design, Synthesis and Structure–Anxiolytic Activity Relationship

  • Tatiana A. Gudasheva,
  • Olga A. Deeva,
  • Andrey S. Pantileev,
  • Grigory V. Mokrov,
  • Inna V. Rybina,
  • Milada A. Yarkova and
  • Sergei B. Seredenin

4 November 2020

The translocator protein (TSPO, 18 kDa) plays an important role in the synthesis of neurosteroids by promoting the transport of cholesterol from the outer to the inner mitochondrial membrane, which is the rate-limiting step in neurosteroidogenesis. S...

  • Article
  • Open Access
47 Citations
8,516 Views
15 Pages

CRISPR-Cas9 Mediated TSPO Gene Knockout alters Respiration and Cellular Metabolism in Human Primary Microglia Cells

  • Vladimir M. Milenkovic,
  • Dounia Slim,
  • Stefanie Bader,
  • Victoria Koch,
  • Elena-Sofia Heinl,
  • David Alvarez-Carbonell,
  • Caroline Nothdurfter,
  • Rainer Rupprecht and
  • Christian H. Wetzel

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, prolifer...

  • Article
  • Open Access
6 Citations
2,627 Views
12 Pages

Feasibility of TSPO-Specific Positron Emission Tomography Radiotracer for Evaluating Paracetamol-Induced Liver Injury

  • Daehee Kim,
  • Byung Seok Moon,
  • Sun Mi Park,
  • Sang Ju Lee,
  • Seo Young Kang,
  • Sanghui Park,
  • Seung Jun Oh,
  • Bom Sahn Kim and
  • Hai-Jeon Yoon

10 September 2021

Macrophages are activated during the early phase of paracetamol-induced liver injury (PLI). [18F]GE180 is a radiolabeled ligand that recognizes the macrophage translocator protein (TSPO). In this study, we evaluated the feasibility of a TSPO-specific...

  • Article
  • Open Access
6 Citations
3,694 Views
8 Pages

14 September 2020

The impact of ligands of the 18 kDa translocator protein (TSPO) on the release of chemokines is not vastly investigated. In the present study, we assessed the effect of our novel TSPO ligands 2-Cl-MGV-1 and 2,4-Di-Cl-MGV-1 compared to the classical T...

  • Article
  • Open Access
3,004 Views
17 Pages

The Traumatic Inoculation Process Affects TSPO Radioligand Uptake in Experimental Orthotopic Glioblastoma

  • Lukas Gold,
  • Enio Barci,
  • Matthias Brendel,
  • Michael Orth,
  • Jiying Cheng,
  • Sabrina V. Kirchleitner,
  • Laura M. Bartos,
  • Dennis Pötter,
  • Maximilian A. Kirchner and
  • Adrien Holzgreve
  • + 15 authors

Background: The translocator protein (TSPO) has been proven to have great potential as a target for the positron emission tomography (PET) imaging of glioblastoma. However, there is an ongoing debate about the potential various sources of the TSPO PE...

  • Article
  • Open Access
45 Citations
7,170 Views
16 Pages

24 November 2018

Choroidal endothelial cells supply oxygen and nutrients to retinal pigment epithelial (RPE) cells and photoreceptors, recycle metabolites, and dispose of metabolic waste through the choroidal blood circulation. Death of the endothelial cells of the c...

  • Article
  • Open Access
20 Citations
10,219 Views
18 Pages

Synthesis, Characterization, and Cytotoxicity of the First Oxaliplatin Pt(IV) Derivative Having a TSPO Ligand in the Axial Position

  • Salvatore Savino,
  • Nunzio Denora,
  • Rosa Maria Iacobazzi,
  • Letizia Porcelli,
  • Amalia Azzariti,
  • Giovanni Natile and
  • Nicola Margiotta

The first Pt(IV) derivative of oxaliplatin carrying a ligand for TSPO (the 18-kDa mitochondrial translocator protein) has been developed. The expression of the translocator protein in the brain and liver of healthy humans is usually low, oppositely t...

  • Article
  • Open Access
5 Citations
4,169 Views
17 Pages

Neurogenic Potential of the 18-kDa Mitochondrial Translocator Protein (TSPO) in Pluripotent P19 Stem Cells

  • Laura González-Blanco,
  • Juan Carlos Bermejo-Millo,
  • Gabriela Oliveira,
  • Yaiza Potes,
  • Eduardo Antuña,
  • Iván Menéndez-Valle,
  • Ignacio Vega-Naredo,
  • Ana Coto-Montes and
  • Beatriz Caballero

17 October 2021

The 18-kDa translocator protein (TSPO) is a key mitochondrial target by which different TSPO ligands exert neuroprotective effects. We assayed the neurogenic potential of TSPO to induce the neuronal differentiation of pluripotent P19 stem cells in vi...

  • Systematic Review
  • Open Access
1 Citations
2,900 Views
14 Pages

A Systematic Review on Dementia and Translocator Protein (TSPO): When Nuclear Medicine Highlights an Underlying Expression

  • Miriam Conte,
  • Maria Silvia De Feo,
  • Ferdinando Corica,
  • Joana Gorica,
  • Marko Magdi Abdou Sidrak,
  • Flaminia De Cristofaro,
  • Luca Filippi,
  • Maria Ricci,
  • Giuseppe De Vincentis and
  • Viviana Frantellizzi

26 March 2023

Background: Translocator protein (TSPO) is a neuroinflammation hallmark. Different TSPO affinity compounds have been produced and over time, the techniques of radiolabeling have been refined. The aim of this systematic review is to summarize the deve...

  • Article
  • Open Access
1 Citations
667 Views
15 Pages

TSPO Modulation Prevents Photoreceptor Degeneration and Produces Neuroprotective Effects in an Animal Model of Retinitis Pigmentosa

  • Francesca Corsi,
  • Jacopo Castagnoli,
  • Alessia Galante,
  • Angela Fabiano,
  • Elisa Nuti,
  • Anna Maria Piras,
  • Sabrina Taliani,
  • Ilaria Piano and
  • Claudia Gargini

12 November 2025

The translocator protein (TSPO), an evolutionarily conserved protein located on the outer mitochondrial membrane, is typically expressed at low levels in the central nervous system under normal physiological conditions. However, its expression can in...

  • Article
  • Open Access
11 Citations
3,691 Views
13 Pages

Brain-Derived Neurotrophic Factor (BDNF) and Translocator Protein (TSPO) as Diagnostic Biomarkers for Acute Ischemic Stroke

  • Mayuri N. Tuwar,
  • Wei-Hung Chen,
  • Arthur M. Chiwaya,
  • Hsu-Ling Yeh,
  • Minh H. Nguyen and
  • Chyi-Huey Bai

Brain-derived neurotrophic factor (BDNF) interacts with tropomyosin-related kinase B (TrkB) to promote neuronal growth, survival, differentiation, neurotransmitter release, and synaptic plasticity. The translocator protein (TSPO) is known to be found...

  • Article
  • Open Access
18 Citations
4,007 Views
13 Pages

Potential TSPO Ligand and Photooxidation Quencher Isorenieratene from Arctic Ocean Rhodococcus sp. B7740

  • Yashu Chen,
  • Mengyao Guo,
  • Jifang Yang,
  • Jigang Chen,
  • Bijun Xie and
  • Zhida Sun

29 May 2019

Due to its special aromatic structure, isorenieratene is thought to be an active natural antioxidant and photo/UV damage inhibitor. In this work, isorenieratene that was extracted from Rhodococcus sp. B7740 isolated from the Arctic Ocean, showed exce...

  • Article
  • Open Access
2,776 Views
22 Pages

TSPO Ligand 2-Cl-MGV-1 Mitigates Traumatic Brain Injury (TBI) in a Mouse Model

  • Nasra Yasin,
  • Leo Veenman,
  • Beatriz Caballero,
  • Nidal Zeineh,
  • Laura Gonzalez-Blanco,
  • Abraham Weizman and
  • Moshe Gavish

In this study, we assessed the ability of 2-Cl-MGV-1 (2-chlorophenyl quinazolin-4-yl, dimethyl carbamate), a ligand of the 18 kDa mitochondrial translocator protein (TSPO), to mitigate brain damage in a mouse model of traumatic brain injury (TBI). TS...

  • Article
  • Open Access
2,221 Views
26 Pages

A Comprehensive Functional Investigation of the Human Translocator Protein 18 kDa (TSPO) in a Novel Human Neuronal Cell Knockout Model

  • Stefanie Bader,
  • Tatjana Jahner,
  • Anett Dörfelt,
  • Doris Melchner,
  • Iseline Cardon,
  • Heiko I. Siegmund,
  • Christoph Brochhausen,
  • Rainer Rupprecht,
  • Vladimir M. Milenkovic and
  • Christian H. Wetzel

29 November 2024

The translocator protein 18 kDa (TSPO) is a multifunctional outer mitochondrial membrane protein associated with various aspects of mitochondrial physiology and multiple roles in health and disease. Here, we aimed to analyse the role of TSPO in the r...

  • Article
  • Open Access
3 Citations
2,876 Views
21 Pages

The TSPO Ligands MGV-1 and 2-Cl-MGV-1 Differentially Inhibit the Cigarette Smoke-Induced Cytotoxicity to H1299 Lung Cancer Cells

  • Nidal Zeineh,
  • Rafael M. Nagler,
  • Martin Gabay,
  • Fadi Obeid,
  • Meygal Kahana,
  • Abraham Weizman and
  • Moshe Gavish

TSPO is involved in cigarette smoke (CS)-induced cellular toxicity, which may result in oral and pulmonary diseases and lung cancer. H1299 lung cancer cells were exposed directly to CS. The H1299 cells were pretreated with our TSPO ligands MGV-1 and...

  • Review
  • Open Access
154 Citations
13,340 Views
37 Pages

Translocator Protein-18 kDa (TSPO) Positron Emission Tomography (PET) Imaging and Its Clinical Impact in Neurodegenerative Diseases

  • Anne-Claire Dupont,
  • Bérenger Largeau,
  • Maria Joao Santiago Ribeiro,
  • Denis Guilloteau,
  • Claire Tronel and
  • Nicolas Arlicot

In vivo exploration of activated microglia in neurodegenerative diseases is achievable by Positron Emission Tomography (PET) imaging, using dedicated radiopharmaceuticals targeting the translocator protein-18 kDa (TSPO). In this review, we emphasized...

  • Article
  • Open Access
14 Citations
6,798 Views
10 Pages

Synthesis and Evaluation of Tricarbonyl 99mTc-Labeled 2-(4-Chloro)phenyl-imidazo[1,2-a]pyridine Analogs as Novel SPECT Imaging Radiotracer for TSPO-Rich Cancer

  • Ji Young Choi,
  • Rosa Maria Iacobazzi,
  • Mara Perrone,
  • Nicola Margiotta,
  • Annalisa Cutrignelli,
  • Jae Ho Jung,
  • Do Dam Park,
  • Byung Seok Moon,
  • Nunzio Denora and
  • Byung Chul Lee
  • + 1 author

The 18-kDa translocator protein (TSPO) levels are associated with brain, breast, and prostate cancer progression and have emerged as viable targets for cancer therapy and imaging. In order to develop highly selective and active ligands with a high af...

  • Article
  • Open Access
32 Citations
5,385 Views
14 Pages

Inhibitory Effects of the Two Novel TSPO Ligands 2-Cl-MGV-1 and MGV-1 on LPS-induced Microglial Activation

  • Sheelu Monga,
  • Rafi Nagler,
  • Rula Amara,
  • Abraham Weizman and
  • Moshe Gavish

22 May 2019

The 18 kDa translocator protein (TSPO) ligands 2-Cl-MGV-1 and MGV-1 can attenuate cell death of astrocyte-like cells (U118MG) and induce differentiation of neuronal progenitor cells (PC-12). Lipopolysaccharide (LPS) is a bacterial membrane endotoxin...

  • Article
  • Open Access
10 Citations
4,139 Views
11 Pages

Astroglial Connexin 43 Deficiency Protects against LPS-Induced Neuroinflammation: A TSPO Brain µPET Study with [18F]FEPPA

  • Nicolas Vignal,
  • Anne-Cécile Boulay,
  • Carine San,
  • Martine Cohen-Salmon,
  • Nathalie Rizzo-Padoin,
  • Laure Sarda-Mantel,
  • Xavier Declèves,
  • Salvatore Cisternino and
  • Benoît Hosten

7 February 2020

Astroglial connexin 43 (Cx43) has been recognized as a crucial immunoregulating factor in the brain. Its inactivation leads to a continuous immune recruitment, cytokine expression modification and a specific humoral autoimmune response against the as...

  • Article
  • Open Access
3 Citations
3,299 Views
15 Pages

Synthesis, In Silico and In Vitro Characterization of Novel N,N-Substituted Pyrazolopyrimidine Acetamide Derivatives for the 18KDa Translocator Protein (TSPO)

  • Jaekyung Park,
  • Sobia Wasim,
  • Jae Ho Jung,
  • Mi-hyun Kim,
  • Byung Chul Lee,
  • Mohammad Maqusood Alam and
  • Sang-Yoon Lee

11 April 2023

The translocator protein (TSPO) is an interesting biological target for molecular imaging and therapy because the overexpression of TSPO is associated with microglial activation caused by neuronal damage or neuroinflammation, and these activated micr...

  • Article
  • Open Access
5 Citations
3,649 Views
19 Pages

Synthesis and Characterization of a “Clickable” PBR28 TSPO-Selective Ligand Derivative Suitable for the Functionalization of Biodegradable Polymer Nanoparticles

  • Renato Auriemma,
  • Mattia Sponchioni,
  • Umberto Capasso Palmiero,
  • Giacomo Rossino,
  • Arianna Rossetti,
  • Andrea Marsala,
  • Simona Collina,
  • Alessandro Sacchetti,
  • Davide Moscatelli and
  • Marco Peviani

28 June 2021

Reactive microgliosis is a pathological hallmark that accompanies neuronal demise in many neurodegenerative diseases, ranging from acute brain/spinal cord injuries to chronic diseases, such as amyotrophic lateral sclerosis (ALS), Alzheimer’s disease...

  • Article
  • Open Access
304 Views
17 Pages

Exploring the Role of TSPO-PET Imaging Among MRI-Negative Patients with Temporal Lobe Epilepsy: From the Perspective of Heterogeneity

  • Yuncan Chen,
  • Jing Wang,
  • Shimin Xu,
  • Qinyue Wang,
  • Shuhao Mei,
  • Jiaying Lu,
  • Yiqiao Wang,
  • Huamei Lin,
  • Dongyan Wu and
  • Xunyi Wu
  • + 4 authors

22 February 2026

Background/Objectives: This study explored the heterogeneous distribution pattern of translocator protein 18kDa (TSPO)-PET/MRI using radioligand [18F] DPA-714 in temporal lobe epilepsy patients and identified clinical factors influencing imaging outc...

  • Article
  • Open Access
33 Citations
5,811 Views
14 Pages

The 18 kDa Translocator Protein (TSPO) is a marker for microglial activation as its expression is enhanced in activated microglia during neuroinflammation. TSPO ligands can attenuate neuroinflammation and neurotoxicity. In the present study, we exami...

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