title: Targeting the 18-kDa translocator protein: recent perspectives for neuroprotection.
abstract: The translocator protein (TSPO, 18 kDa), mainly localized in the outer mitochondrial membrane of steroidogenic tissues, is involved in several cellular functions. TSPO level alterations have been reported in a number of human disorders, particularly in cancer, psychiatric and neurological diseases. In the central nervous system (CNS), TSPO is usually expressed in glial cells, but also in some neuronal cell types. Interestingly, the expression of TSPO on glial cells rises after brain injury and increased TSPO expression is often observed in neurological disorders, gliomas, encephalitis and traumatic injury. Since TSPO is up-regulated in brain diseases, several structurally different classes of ligands targeting TSPO have been described as potential diagnostic or therapeutic agents. Recent researches have reported that TSPO ligands might be valuable in the treatment of brain diseases. This review focuses on currently available TSPO ligands, as useful tools for the treatment of neurodegeneration, neuro-inflammation and neurotrauma.
authors.affiliation: Department of Pharmacy, University of Pisa, Via Bonanno 6, 56126 Pisa, Italy.
authors.forename: Eleonora
authors.initials: E
authors.lastname: Da Pozzo
authors.affiliation: Department of Pharmacy, University of Pisa, Via Bonanno 6, 56126 Pisa, Italy.
authors.forename: Chiara
authors.initials: C
authors.lastname: Giacomelli
authors.affiliation: Department of Pharmacy, University of Pisa, Via Bonanno 6, 56126 Pisa, Italy.
authors.forename: Elisabetta
authors.initials: E
authors.lastname: Barresi
authors.affiliation: Department of Pharmacy, University of Pisa, Via Bonanno 6, 56126 Pisa, Italy.
authors.forename: Barbara
authors.initials: B
authors.lastname: Costa
authors.affiliation: Department of Pharmacy, University of Pisa, Via Bonanno 6, 56126 Pisa, Italy.
authors.forename: Sabrina
authors.initials: S
authors.lastname: Taliani
authors.affiliation: Department of Pharmacy, University of Pisa, Via Bonanno 6, 56126 Pisa, Italy.
authors.forename: Federico Da Settimo
authors.initials: Fda S
authors.lastname: Passetti
authors.affiliation: Department of Pharmacy, University of Pisa, Via Bonanno 6, 56126 Pisa, Italy claudia.martini@unipi.it.
authors.forename: Claudia
authors.initials: C
authors.lastname: Martini
mesh_terms: D000818:Animals; D001927:Brain Diseases / Q000188:drug therapy* / Q000378:metabolism; D006801:Humans; D008024:Ligands; D058990:Molecular Targeted Therapy; D009457:Neuroglia / Q000378:metabolism; D009474:Neurons / Q000378:metabolism; D018696:Neuroprotective Agents / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D018079:Receptors, GABA / Q000378:metabolism*; D015398:Signal Transduction / Q000187:drug effects; D015854:Up-Regulation
chemical_list: D008024:Ligands; D018696:Neuroprotective Agents; D018079:Receptors, GABA; C499229:TSPO protein, human
keywords: central nervous system diseases; neuro-inflammation; neurodegeneration; neurotrauma; translocator protein; translocator protein (TSPO) ligand