An orally active inhibitor of sPLA2-IIA
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Secreted phospholipases A2 (sPLA2s) are a diverse family of low molecular weight PLA2s with tissue-specific expression patterns and actions. The group IIA sPLA2 (sPLA2-IIA) was originally purified from platelets and exudates from patients with rheumatoid arthritis. Its expression can be induced by inflammatory mediators, and mouse studies suggest that it may play roles in colorectal polyposis, atherosclerosis, and bacterial infections. sPLA2 inhibitor is an orally active inhibitor of sPLA2-IIA. It protects against intestinal reperfusion injury in rats when given at 10 mg/kg orally. sPLA2 inhibitor also attenuates NF-κB signaling in lung cancer cells and protects against diet-induced metabolic syndrome in rats.
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