Translocator protein (TSPO) ligands for the diagnosis or treatment of neurodegenerative diseases: a patent review (2010 – 2015; part 2). (1st November 2016)

• Record Type: Journal Article
• Authors: Kim, TaeHun; Pae, Ae Nim
• Is Part Of: Expert opinion on therapeutic patents. Volume 26:Number 11(2016:Nov.)
• Page Start: 1353
• Page End: 1366
• Publication Date: 2016-11-01
• Subjects: TSPO -- PBR -- neurodegenerative disease -- neuroinflammation -- FGIN-1-27 -- SSR180575 -- TRO19622 -- GE-180; Drugs -- Patents -- Periodicals; 615.10272
• DOI: 10.1080/13543776.2016.1230605
• Languages: English
• ISSNs: 1354-3776

Abstract

ABSTRACT: Introduction: The 18-k Da translocator protein (TSPO) has been highlighted as a potential drug target in diverse neurodegenerative diseases because the up-regulation of TSPO in the CNS is related to neuroinflammation. Diverse TSPO ligands are currently in clinical trials or are under development at the preclinical stage for the treatment and/or diagnosis of neurodegenerative processes. These TSPO ligands may shed light on novel therapeutics for neurodegenerative diseases in the near future. Areas covered: This review describes TSPO ligands that have been patented from 2010 to 2015. Numerous indole-derived TSPO ligands will be analyzed on the basis of their TSPO affinities. Furthermore, cholesterol-like compounds and miscellaneous TSPO ligands will be summarized along with their pharmaceutical uses. Expert opinion: Diverse TSPO ligands have demonstrated their biological efficacies in experimental models of neurodegenerative diseases, and some of them are now in clinical trials. The indole-derived TSPO ligands can be highlighted as efficient diagnostic agents because they have high selectivity and affinity for TSPO. Moreover, one potent cholesterol-like TSPO ligand has been described as a neuroprotective compound. Therefore, additional preclinical and clinical studies for highly potent TSPO ligands are recommended for the successful pharmacological application of TSPO ligands.