Translocator protein (TSPO) ligands for the diagnosis or treatment of neurodegenerative diseases: a patent review (2010 - 2015; part 2).
The 18-kDa 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.
a Convergence Research Center for Diagnosis, Treatment and Care System of Dementia , Korea Institute of Science and Technology , Seoul , Republic of Korea.|b Biological Chemistry , Korea University of Science and Technology , Daejon , Republic of Korea.
TaeHun
T
Kim
a Convergence Research Center for Diagnosis, Treatment and Care System of Dementia , Korea Institute of Science and Technology , Seoul , Republic of Korea.|b Biological Chemistry , Korea University of Science and Technology , Daejon , Republic of Korea.
Ae Nim
AN
Pae
D000818:Animals; D002784:Cholesterol / Q000378:metabolism; D004195:Disease Models, Animal; D015195:Drug Design; D006801:Humans; D007211:Indoles / Q000737:chemistry / Q000494:pharmacology; D008024:Ligands; D019636:Neurodegenerative Diseases / Q000175:diagnosis / Q000188:drug therapy* / Q000503:physiopathology; D010330:Patents as Topic; D018079:Receptors, GABA / Q000378:metabolism*
D007211:Indoles; D008024:Ligands; D018079:Receptors, GABA; C499229:TSPO protein, human; D002784:Cholesterol
FGIN-1-27; GE-180; PBR; SSR180575; TRO19622; TSPO; neurodegenerative disease; neuroinflammation