Synonyms: TH-5487
Compound class:
Synthetic organic
Comment: TH5487 is a selective, active-site inhibitor of 8-oxoguanine DNA glycosylase (OGG1) [2]. OGG1 repairs 8-hydroxy-2′-deoxyguanosine (8-oxoG) DNA defects that can be induced by reactive oxygen species (ROS) at sites of inflammation. TH5487 inhibits OGG1-mediated proinflammatory activity in allergic states. In a mouse model of allergic airway inflammation TH5487 reduced NF-κB-mediated expression of proinflammatory cytokines/chemokines and inhibited immune cell recruitment into the lungs with an associated reduction in goblet cell hyperplasia and mucus production [1].
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References |
1. Tanner L, Jesper B, Ravi BKV, Lang P, Caijuan D, Olov W, Kalderén C, Helleday T, Boldogh I, Adner M et al.. (2022)
Pharmacological OGG1 inhibition decreases murine allergic airway inflammation. Frontiers in Pharmacology, 13 Epub ahead of print. DOI: 10.3389/fphar.2022.999180 |
2. Visnes T, Cázares-Körner A, Hao W, Wallner O, Masuyer G, Loseva O, Mortusewicz O, Wiita E, Sarno A, Manoilov A et al.. (2018)
Small-molecule inhibitor of OGG1 suppresses proinflammatory gene expression and inflammation. Science, 362 (6416): 834-839. [PMID:30442810] |