RORγt is a T cell specific isoform of ROR that is a key transcription factor for initiating the differentiation of Th17 and Tc17 cells. SR0987 (303126-97-8) is a RORγt agonist that drives proliferation of Th17 cells and decreases levels of the immune checkpoint protein PD-1. In a Ga14 UAS-Luc cotransfection system, SR0987 induced reporter gene expression (EC50 = 800nM). Treatment of human Jurkat T cells with SR0987 resulted in decreased cell surface PD-1 expression. RORγt agonists may synergize with current anti-PD-1 therapy and represent a new potential class of cancer immunotherapeutic.
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