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Irreversible S1PR2 Antagonists for the Treatment of Inflammation and Fibrosis
Lead compounds with demonstrated efficacy in the mouse bile duct ligation model
Background
- Sphingosine-1-phosphate (S1P) is a bioactive lipid that regulates many physiological (and pathophysiological) processes
- The S1PR2 receptor is an abundant GPCR widely expressed in the endothelium, in addition to fibrogenic and immune cells, and is upregulated by inflammation
- S1PR2 modulates several metabolic pathways in the liver, including regeneration after hepatic injury
- S1PR2 is believed to be one of the key drivers of tissue injury and fibrosis, and is thus a promising therapeutic target
- Unmet Need: Novel anti-fibrotic agents that prevent disease progression by targeting pro-fibrotic factors such as S1PR2
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