Identification of bioactive compounds modulating STING activation

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Fig. 1. Identification of bioactive compounds modulating STING activation. Identification of bioactive compounds modulating STING activation. (A) Heatmap of STING activity changes based on IFNβ release from iBMDMs after 3′3′-cGAMP (10 μg/ml, 16 hours) stimulation in the absence or presence of 464 bioactive compounds (10 μM). (B) Structure of the compound identified to inhibit (blue) or promote (red) STING activity. (C to E) IFNβ release assayed using enzyme-linked immunosorbent assay (ELISA) from iBMDMs (C), pPMs (D), and pPBMCs (E) treated with 3′3′-cGAMP (10 μg/ml) in the absence or presence of indicated bioactive compounds (10 μM) for 16 hours [n = 3; data are means ± SD; *P < 0.05 versus 3′3′-cGAMP group, analysis of variance (ANOVA) least significant difference (LSD) test]. (F) Heatmap of STING activity changes as judged by IFNβ release from iBMDMs after 3′3′-cGAMP (10 μg/ml, 16 hours) stimulation in the absence or presence of 174 signaling modulating compounds. The top five negative (inhibitory) and positive (agonistic) regulators are noted. Ling Zeng et al., Sci Transl Med 2017;9:eaan5689 Published by AAAS