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Current Pharmaceutical Design


ISSN (Print): 1381-6128
ISSN (Online): 1873-4286

Review Article

The Ligands of Translocator Protein: Design and Biological Properties

Author(s): Grigory V. Mokrov, Olga A. Deeva and Tatiana A. Gudasheva*

Volume 27 , Issue 2 , 2021

Published on: 03 September, 2020

Page: [217 - 237] Pages: 21

DOI: 10.2174/1381612826666200903122025

Price: $65


In 2020, it is already 43 years since Braestrup and Squires discovered 18 kDa translocator protein (TSPO), known until 2006 as "peripheral benzodiazepine receptor". During this time, the functions of this receptor, which is located on the outer membrane of mitochondria, were studied in detail. One of the key functions of TSPO is the transfer of cholesterol from the outer to the inner mitochondrial membrane, which is the limiting stage in the synthesis of neurosteroids. TSPO is also involved in the transport of porphyrins, mitochondrial respiration, the opening of mitochondrial pores, apoptosis and cell proliferation. This review presents current information on the structure of TSPO, the mechanism of its participation in neurosteroidogenesis, as well as endogenous and synthetic TSPO ligands. Particular emphasis is placed on the analysis of approaches to the design of synthetic ligands and their neuropsychotropic activity in vitro and in vivo. The presented review demonstrates the promise of constructing new neuropsychotropic drugs in the series of TSPO ligands.

Keywords: 18 kDa translocator protein TSPO, TSPO ligands, neuropsychotropic activity, drug design, neurosteroids, cholesterol.

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