Fig. 2: Identification of prostaglandin D2 as an allosteric inhibitor of A2AR. | Communications Chemistry

Fig. 2: Identification of prostaglandin D2 as an allosteric inhibitor of A2AR.

From: Systematic metabolite screening identifies functional regulators of the adenosine A2A receptor

Fig. 2: Identification of prostaglandin D2 as an allosteric inhibitor of A2AR.

a, b Metabolites were screened for (a) activation at 10 μM or (b) inhibition at 100 μM. Data was analyzed by one-way ANOVA and adjusted using Dunnett’s multiple comparisons test. For activation, (F(10,22) = 40.74, p < 0.0001), For SAH, p < 0.0001. For inhibition, F(10,22) = 151.9, p < 0.0001). For ZM and PGD2, p < 0.0001 (c) GTP hydrolysis assay demonstrating sustained inhibition of A2AR in the presence of 500 μM PGD2. (d) PGD2 inhibition in HEK293 cells stably expressing A2AR. a–d All data points shown as mean ± SD, n = 3 technical replicates, ****p < 0.0001.

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