Translocator Protein (TSPO)

Dear Colleagues,

Decades of study on the 18-kDa mitochondrial translocator protein (TSPO), first discovered in the late 1977 as an alternative binding site for the benzodiazepine diazepam in the kidneys, have revealed that this protein participates in a variety of cellular functions, including cholesterol transport, steroid hormone synthesis, mitochondrial respiration, permeability transition pore opening, apoptosis, and cell proliferation. In accordance with TSPO's diverse functions, changes in TSPO expression have been linked to multiple diseases, from cancer to endocrine and neurological diseases. Thus, TSPO has become an extremely attractive subcellular target for: (1) the early detection of disease states that involve the overexpression of this protein; (2) selective mitochondrial drug delivery.

Investigation of the functions of this protein, both in vitro and in vivo, has been mainly carried out using high-affinity ligands, such as isoquinoline carboxamides (e.g., PK 11195) and benzodiazepines (e.g., Ro5-4864). For instance, PK 11195 and Ro5-4864 have been used to explore TSPO distribution and function in various tissues and pathologies, thus allowing for the mapping of the “peripheral binding site” in almost every tissue examined. In time, the number of structurally diverse TSPO drug ligands investigated has increased steeply, thus highlighting the great interest of the scientific community in understanding the functions of this translocator protein in both normal conditions and pathological states.

This Special Issue will consist of reviews and primary data manuscripts, and will focus on: (1) new potent and selective TSPO ligands; (2) the use of ligands as imaging tools for the early diagnosis of diseases characterized by the high expression of TSPO, such as neuroinflammation and TSPO-rich cancers; (3) TSPO targeted nanocarriers that deliver therapeutics and diagnostics; (4) TSPO ligands that could be used to prepare coordination complexes of metallodrugs, for use in diagnosis and therapy; (5) TSPO ligands as pro-apoptotic agents that are potentially useful for the treatment of cancers; and (6) in vitro and in vivo investigations of the ability of TSPO ligands to affect steroidogenesis.

Prof. Giovanni Natile
Prof. Dr. Nunzio Denora
Guest Editors

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