期刊
EXPERT OPINION ON THERAPEUTIC PATENTS
卷 26, 期 11, 页码 1325-1351出版社
TAYLOR & FRANCIS LTD
DOI: 10.1080/13543776.2016.1230606
关键词
TSPO; PBR; neurodegenerative disease; neuroinflammation; PK 11195; Ro5-4864; emapunil; alpidem; DAA1106; PBR28
资金
- National Research Council of Science & Technology (NST) - Korea government (MSIP) [CRC-15-04-KIST, 2N41660]
- Korea Institute of Science and Technology [2E26650]
- Ministry of Science, ICT & Future Planning, Republic of Korea [2E26650] Funding Source: Korea Institute of Science & Technology Information (KISTI), National Science & Technology Information Service (NTIS)
Introduction: The translocator protein (TSPO) is an emerging target in diverse neurodegenerative diseases. Up-regulated TSPO in the central nervous system (CNS) appears to be involved in neuroinflammatory processes; therefore, the development of potent TSPO ligands is a promising method for alleviating or imaging patients with neurodegenerative diseases. Areas covered: This review will provide an overview of recently developed TSPO ligands patented from 2010 to 2015. Part 1 will present a summary focusing on TSPO ligands other than indole-based or cholesterol-like compounds, which will be discussed in part 2. Part 1 covers diverse benzodiazepine-derived analogues such as isoquinoline carboxamides and aryloxyanilides. Moreover, bicyclic ring structures such as imidazopyridine, pyrazolopyrimidine, and phenylpurine will be highlighted as promising scaffolds for TSPO ligands. A brief analysis of currently reported TSPO structures will also be covered in part 1. Expert opinion: Although the underlying pharmacological mechanism of TSPO remains to be elucidated, several TSPO ligands have shown therapeutic efficacy in experimental animal models of neurodegenerative diseases. In addition, radioactive TSPO ligands have been extensively studied for the diagnosis of neurodegenerative processes. Thus, further studies on both the basic and applied mechanisms of TSPO are warranted in the pursuit of successful pharmacological applications of TSPO ligands.
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