Cellular sources of TSPO expression in healthy and diseased brain
The 18 kDa translocator protein (TSPO) is a highly conserved protein located in the outer
mitochondrial membrane. TSPO binding, as measured with positron emission tomography …
mitochondrial membrane. TSPO binding, as measured with positron emission tomography …
The alpha keto amide moiety as a privileged motif in medicinal chemistry: current insights and emerging opportunities
M Robello, E Barresi, E Baglini, S Salerno… - Journal of Medicinal …, 2021 - ACS Publications
Over the years, researchers in drug discovery have taken advantage of the use of privileged
structures to design innovative hit/lead molecules. The α-ketoamide motif is found in many …
structures to design innovative hit/lead molecules. The α-ketoamide motif is found in many …
Unbiased molecular dynamics of 11 min timescale drug unbinding reveals transition state stabilizing interactions
Ligand (un) binding kinetics is being recognized as a determinant of drug specificity and
efficacy in an increasing number of systems. However, the calculation of kinetics and the …
efficacy in an increasing number of systems. However, the calculation of kinetics and the …
Translocator protein (18 kDa): an update on its function in steroidogenesis
Translocator protein (18 kDa)(TSPO) is a ubiquitous mitochondrial protein. Studies of its
responses to drug and endogenous ligands have shown TSPO to be involved either directly …
responses to drug and endogenous ligands have shown TSPO to be involved either directly …
Microglial pro-inflammatory and anti-inflammatory phenotypes are modulated by translocator protein activation
E Da Pozzo, C Tremolanti, B Costa… - International journal of …, 2019 - mdpi.com
A key role of the mitochondrial Translocator Protein 18 KDa (TSPO) in neuroinflammation
has been recently proposed. However, little is known about TSPO-activated pathways …
has been recently proposed. However, little is known about TSPO-activated pathways …
TSPO: an evolutionarily conserved protein with elusive functions
F Bonsack, S Sukumari-Ramesh - International journal of molecular …, 2018 - mdpi.com
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 …
tissue binding sites for benzodiazepines, and was formerly called the peripheral …
An update into the medicinal chemistry of translocator protein (TSPO) ligands
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 …
alternative binding site for the benzodiazepine diazepam. It is an evolutionary well …
Differential effects of TSPO ligands on mitochondrial function in mouse microglia cells
The translocator protein 18 kDa (TSPO), initially characterized as peripheral
benzodiazepine receptor, is a conserved outer mitochondrial membrane protein, implicated …
benzodiazepine receptor, is a conserved outer mitochondrial membrane protein, implicated …
Protein–ligand (un) binding kinetics as a new paradigm for drug discovery at the crossroad between experiments and modelling
In the last three decades, protein and nucleic acid structure determination and
comprehension of the mechanisms, leading to their physiological and pathological …
comprehension of the mechanisms, leading to their physiological and pathological …
Translocator protein ligand protects against neurodegeneration in the MPTP mouse model of Parkinsonism
J Gong, ÉM Szego, A Leonov, E Benito… - Journal of …, 2019 - Soc Neuroscience
Parkinson's disease is the second most common neurodegenerative disease, after
Alzheimer's disease. Parkinson's disease is a movement disorder with characteristic motor …
Alzheimer's disease. Parkinson's disease is a movement disorder with characteristic motor …