Translocator protein TSPO 18 kDa and its ligands: a promising approach to the creation of new neuropsychotropic drug

Abstract

Resume. It is 41 years in 2018 since Braestrup and Squires opened translocator protein 18 kDa TSPO, known until 2006 as the peripheral benzodiazepine receptor (PBR). The functions of this receptor, which is one of the most important component of the outer mitochondrial membrane, have been studied in detail during this time. One of the key functions of TSPO is the transfer of cholesterol from the outer to the inner membrane of mitochondria, which is the limiting step in the synthesis of neurosteroids. In addition, TSPO is involved in porphyrin transport, mitochondrial respiration, the opening of mitochondrial pores, apoptosis and cell proliferation. This review presents the modern views on the structure of TSPO, the mechanism of it participation in neurosteroidogenesis and the endogenous and synthetic ligands of TSPO. Particular emphasis is placed on the analysis of approaches to the design of synthetic ligands and their neuropsychotropic activity in vitro and in vivo. This review demonstrates the prospects of new neuropsychotic drugs design among TSPO ligands.

Keywords

• транслокаторный белок tspo 18 кда
• лиганды tspo
• нейропсихотропная активность
• дизайн новых лекарственных средств
• нейростероиды
• translocator protein tspo 18 kda
• tspo ligands
• neuropsychotropic activity
• design of new drugs
• neurosteroids