ArticleBiochemistry2013
Characterization and modeling of the oligomeric state and ligand binding behavior of purified translocator protein 18 kDa from Rhodobacter sphaeroides.
Article in Biochemistry, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 34 papers.
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Who cites it
34 citing papers in PubMed, 58 citations in OpenAlex.
- TSPO in systemic-ocular immunometabolic crosstalk: mechanisms and therapeutic implications.Frontiers in immunology · 2026Review
- TSPO Ligand 2-Cl-MGV-1 Mitigates Traumatic Brain Injury (TBI) in a Mouse Model.International journal of molecular sciences · 2025Article
- Cholesterol-dependent enzyme activity of human TSPO1.Proceedings of the National Academy of Sciences of the United States of America · 2025Article
- Translocator Protein 18 kDa (TSPO): A Promising Molecular Target for Image-Guided Surgery of Solid Cancers.Advanced pharmaceutical bulletin · 2024Review
- Structural Insights into the Binding and Degradation Mechanisms of Protoporphyrin IX by the Translocator Protein TSPO.JACS Au · 2023Article
- Evidence for crosstalk between the aryl hydrocarbon receptor and the translocator protein in mouse lung epithelial cells.Experimental cell research · 2023Article
- New TSPO Crystal Structures of Mutant and Heme-Bound Forms with Altered Flexibility, Ligand Binding, and Porphyrin Degradation Activity.Biochemistry · 2023Article
- Mitochondrial control of microglial phagocytosis by the translocator protein and hexokinase 2 in Alzheimer's disease.Proceedings of the National Academy of Sciences of the United States of America · 2023Article
- Differential mitochondrial protein interaction profile between human translocator protein and its A147T polymorphism variant.PloS one · 2022Article
- Mitochondrial translocator protein deficiency exacerbates pathology in acute experimental ulcerative colitis.Frontiers in physiology · 2022Article
- TSPO protein binding partners in bacteria, animals, and plants.Journal of bioenergetics and biomembranes · 2021Review
- The Interplay of Cholesterol and Ligand Binding inMolecules (Basel, Switzerland) · 2021Article
- Impact of Cholesterol on the Stability of Monomeric and Dimeric Forms of the Translocator Protein TSPO: A Molecular Simulation Study.Molecules (Basel, Switzerland) · 2020Article
- Combining native and 'omics' mass spectrometry to identify endogenous ligands bound to membrane proteins.Nature methods · 2020Article
- Insight into the Structural Features of TSPO: Implications for Drug Development.Trends in pharmacological sciences · 2020Review
- Combined treatment of AT101 and demethoxycurcumin yields an enhanced anti-proliferative effect in human primary glioblastoma cells.Journal of cancer research and clinical oncology · 2020Article
- AT101-Loaded Cubosomes as an Alternative for Improved Glioblastoma Therapy.International journal of nanomedicine · 2020Article
- Characterization of the High-Affinity Drug Ligand Binding Site of Mouse Recombinant TSPO.International journal of molecular sciences · 2019Article
- Structural Prediction of the Dimeric Form of the Mammalian Translocator Membrane Protein TSPO: A Key Target for Brain Diagnostics.International journal of molecular sciences · 2018Article
- TSPO: An Evolutionarily Conserved Protein with Elusive Functions.International journal of molecular sciences · 2018Review
Corrections and comments
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Authors and funding
4 authors at 2 institutions in 1 country.
Funding
Abstract
Translocator Protein 18 kDa (TSPO), previously known as the peripheral-type benzodiazepine receptor (PBR), is a mitochondrial outer membrane protein that has been identified as a key player in cholesterol and porphyrin transport, apoptotic signaling, and cancer development, as well as neurological inflammation and disease. Despite a number of TSPO ligands whose effects have been studied with respect to these varied biological activities, the nature of their interactions with TSPO and the molecular mechanism of their effects remain controversial, in part because of the lack of an atomic-resolution structure. We expressed and purified the homologue of mammalian TSPO from Rhodobacter sphaeroides (RsTSPO), as well as a mutant form in a proposed drug binding loop, RsTSPOW38C. We characterized their binding behaviors with endogenous ligands and a series of compounds that affect apoptosis by using a sensitive tryptophan fluorescence quenching assay. Our results show that RsTSPO behaves as a dimer in the purified state and binds with low micromolar affinity to many of these ligands, including retinoic acid, curcumin, and a known Bcl-2 inhibitor, gossypol, suggesting a possible direct role for TSPO in their regulation of apoptosis. A computational model of the RsTSPO dimer is constructed using EM-Fold, Rosetta, and a cryo-electron microscopy density map. Binding behaviors of known ligands are discussed in the context of the model with respect to regions that may be involved in binding.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.