Residence Time, a New parameter to Predict Neurosteroidogenic Efficacy of Translocator Protein (TSPO) Ligands: the Case Study of N,N‐Dialkyl‐2‐arylindol‐3‐ylglyoxylamides
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DOI: 10.1002/cmdc.201700220
Abstract: Targeting the biosynthetic pathway of neuroactive steroids with specific 18 kDa translocator protein (TSPO) ligands may be a viable therapeutic approach for a variety of neurodegenerative and neuropsychiatric diseases. However, the lack of correlation between binding… read more here.
Keywords: residence time; protein tspo; time; efficacy ... See more keywords
Bridging Pharmaceutical Chemistry with Drug and Nanoparticle Targeting to Investigate the Role of the 18‐kDa Translocator Protein TSPO
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DOI: 10.1002/cmdc.201700322
Abstract: An interesting mitochondrial biomarker is the 18‐kDa mitochondrial translocator protein (TSPO). Decades of study have shown that this protein plays an important role in a wide range of cellular functions, including opening of the mitochondrial… read more here.
Keywords: protein; protein tspo; chemistry; translocator protein ... See more keywords
Increased Expression of Translocator Protein (TSPO) Marks Pro-inflammatory Microglia but Does Not Predict Neurodegeneration
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DOI: 10.1007/s11307-017-1099-1
Abstract: PurposeActivation of the innate immune system plays a significant role in pathologies of the central nervous system (CNS). In order to follow disease progression and evaluate effectiveness of potential treatments involved in neuroinflammation, it is… read more here.
Keywords: tspo; protein tspo; translocator protein; expression ... See more keywords
Versatile Dimerisation Process of Translocator Protein (TSPO) Revealed by an Extensive Sampling Based on a Coarse-Grained Dynamics Study
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DOI: 10.1021/acs.jcim.0c00246
Abstract: Translocator protein (TSPO), a mitochondrial membrane protein, has been extensively studied and its role is still debated and continues to be enigmatic. From a structural perspective, despite availability of atomic structures from different species, the… read more here.
Keywords: tspo; protein; protein tspo; translocator protein ... See more keywords
Exploiting the 4-Phenylquinazoline Scaffold for the Development of High Affinity Fluorescent Probes for the Translocator Protein (TSPO).
Sign Up to like & getrecommendations! Published in 2017 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.7b01031
Abstract: The quinazoline class was exploited to search for a new translocator protein (TSPO) fluorescent probe endowed with improved affinity and residence time (RT). Computational studies on an "in-house" collection of quinazoline derivatives, featuring highly steric… read more here.
Keywords: protein tspo; affinity; exploiting phenylquinazoline; fluorescent ... See more keywords
Determination and reduction of translocator protein (TSPO) ligand rs6971 discrimination† †The authors declare no competing interests.
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DOI: 10.1039/c6md00523c
Abstract: The 18 kDa translocator protein (TSPO) is a target for development of diagnostic imaging agents for glioblastoma and neuroinflammation. read more here.
Keywords: translocator protein; reduction translocator; protein tspo; determination reduction ... See more keywords
A Systematic Review on Dementia and Translocator Protein (TSPO): When Nuclear Medicine Highlights an Underlying Expression
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DOI: 10.3390/biom13040598
Abstract: 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… read more here.
Keywords: translocator protein; systematic review; nuclear medicine; protein tspo ... See more keywords
Structural Prediction of the Dimeric Form of the Mammalian Translocator Membrane Protein TSPO: A Key Target for Brain Diagnostics
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DOI: 10.3390/ijms19092588
Abstract: Positron emission tomography (PET) radioligands targeting the human translocator membrane protein (TSPO) are broadly used for the investigations of neuroinflammatory conditions associated with neurological disorders. Structural information on the mammalian protein homodimers—the suggested functional state… read more here.
Keywords: protein; protein tspo; translocator membrane; membrane protein ... See more keywords
Synthesis, In Silico and In Vitro Characterization of Novel N,N-Substituted Pyrazolopyrimidine Acetamide Derivatives for the 18KDa Translocator Protein (TSPO)
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DOI: 10.3390/ph16040576
Abstract: 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 microglia are… read more here.
Keywords: translocator protein; protein tspo; tspo; novel ... See more keywords