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Description: GSK2981278 is a novel potent and selective inverse agonist of retinoid-related orphan receptor gamma (RORy). As a strong RORgamma-selective inverse agonist and modulator, GSK2981278 inhibits the activation of the il17 promoter. GSK2981278 robustly inhibits RORgamma-mediated cytokine production at both the mRNA and protein level. GSK2981278 attenuates inflammation in a mouse model of psoriasis. Topical treatment with GSK2981278 significantly limit Th17-type cytokine expression and should therefore lead to improved clinical outcomes for patients.
References: https://patents.google.com/patent/WO2015061515A1
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