An update into the medicinal chemistry of translocator protein (TSPO) ligands

E Barresi, M Robello, B Costa, E Da Pozzo… - European Journal of …, 2021 - Elsevier
Abstract The Translocator Protein 18 kDa (TSPO) has been discovered in 1977 as an
alternative binding site for the benzodiazepine diazepam. It is an evolutionary well …

[HTML][HTML] Imaging of neuroinflammation in Alzheimer's disease, multiple sclerosis and stroke: Recent developments in positron emission tomography

B Janssen, DJ Vugts, U Funke, GT Molenaar… - … et Biophysica Acta (BBA …, 2016 - Elsevier
Neuroinflammation is thought to play a pivotal role in many diseases affecting the brain,
including Alzheimer's disease, multiple sclerosis and stroke. Neuroinflammation is …

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

J Park, S Wasim, JH Jung, M Kim, BC Lee, MM Alam… - Pharmaceuticals, 2023 - mdpi.com
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 …

Generalization of endothelial modelling of TSPO PET imaging: considerations on tracer affinities

G Rizzo, M Veronese, M Tonietto… - Journal of Cerebral …, 2019 - journals.sagepub.com
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 …

Targeting mitochondria in tumor-associated macrophages using a dendrimer-conjugated TSPO ligand that stimulates antitumor signaling in glioblastoma

A Sharma, K Liaw, R Sharma, AG Thomas… - …, 2020 - ACS Publications
Mitochondria mediate critical cellular processes, including proliferation, apoptosis, and
immune responses; as such, their dysfunction is pathogenic in many neurodegenerative …

Translocator protein (TSPO) ligands for the diagnosis or treatment of neurodegenerative diseases: A patent review (2010–2015; part 1)

TH Kim, AN Pae - Expert opinion on therapeutic patents, 2016 - Taylor & Francis
Introduction: The translocator protein (TSPO) is an emerging target in diverse
neurodegenerative diseases. Up-regulated TSPO in the central nervous system (CNS) …

[HTML][HTML] Targeting glioblastoma through nano-and micro-particle-mediated immune modulation

E Poot, A Maguregui, VG Brunton, D Sieger… - Bioorganic & Medicinal …, 2022 - Elsevier
Glioblastoma Multiforme (GBM) is a multifaceted and complex disease, which has
experienced no changes in treatment for nearly two decades and has a 5-year survival rate …

Translocator protein 18-kDa: a promising target to treat neuroinflammation-related degenerative diseases

C Tremolanti, L Germelli, E Barresi… - Current Medicinal …, 2022 - ingentaconnect.com
In the nervous system, inflammatory responses physiologically occur as defense
mechanisms triggered by damaging events. If improperly regulated, neuroinflammation can …

Privileged scaffolds in medicinal chemistry: Studies on pyrazolo [1, 5-a] pyrimidines on sulfonamide containing Carbonic Anhydrase inhibitors

A Gumus, M Bozdag, A Angeli, TS Peat, F Carta… - Bioorganic & Medicinal …, 2021 - Elsevier
We report for the first time a small series of compounds endowed in vitro with inhibitory
properties for the human (h) expressed Carbonic Anhydrase (CAs, EC 4.2. 1.1) enzymes of …

Synthesis and evaluation of novel potent TSPO PET ligands with 2-phenylpyrazolo [1, 5-a] pyrimidin-3-yl acetamide

VH Tran, H Park, J Park, YD Kwon, S Kang… - Bioorganic & Medicinal …, 2019 - Elsevier
Translocator protein (TSPO) expression is closely related with neuroinflammation and
neuronal damage which might cause several central nervous system diseases. Herein, a …