SLC46A2 is a cGAMP transporter. (A) Effect of sulfasalazine (SSZ)
and methotrexate (MTX) on extracellular cGAMP signaling in CD14+ monocytes. Cells were pretreated with 1 mM SSZ or 500 μM
MTX for 15 min and then treated with 50 μM cGAMP for 2 h. n = 7 individual donors. (B) Diagram illustrating effects
of the SLC19A1 inhibitors SSZ and MTX on extracellular cGAMP signaling
in U937 cells compared to CD14+ monocytes. (C) Microarray
RNA expression levels of genes annotated as plasma membrane transmembrane
transporters in U937 cells compared to CD14+ monocytes.
(D) Effect of SLC46A2 overexpression on extracellular cGAMP signaling.
U937-tet-SLC46A2-FLAG cells were induced with 1 μg/mL doxycycline
(dox) for 24 h, then treated with 50 μM cGAMP for 2 h. n = 9 biological replicates. (E) Schematic illustrating
how cGAMP electroporation bypasses cGAMP transporters. (F) Effect
of SLC46A2 overexpression on intracellular cGAMP signaling. U937-tet-SLC46A2-FLAG
cells were induced with 1 μg/mL dox for 24 h then electroporated
with 100 nM cGAMP for 2 h. n = 2 biological replicates.
(G) Effect of SSZ on SLC46A2 mediated cGAMP signaling. U937-tet-SLC46A2-FLAG
cells were induced with 1 μg/mL dox for 24 h, then pretreated
with 1 mM SSZ for 15 min before treatment with 50 μM cGAMP for
2 h. n = 4 biological replicates. (H–J) U937-tet-SLC46A2FLAG
cells were induced with 1 μg/mL dox for 24 h before treatment
with either 15 μM 2′3′-cGSASMP (H), 15 μM 2′3′-CDAS (I), or 200
μM 3′3′-cGAMP (J) for 2 h. n = 2–3 biological replicates. For parts A–J, the pIRF3
signal was normalized to the tubulin signal, and data are shown as
mean ± SD.