On the G protein-coupling selectivity of the native A2B adenosine receptor.

@article{Gao2018OnTG,
  title={On the G protein-coupling selectivity of the native A2B adenosine receptor.},
  author={Zhan-guo Gao and Asuka Inoue and Kenneth A. Jacobson},
  journal={Biochemical pharmacology},
  year={2018},
  volume={151},
  pages={
          201-213
        }
}
A2B adenosine receptor (A2BAR) activation induces Gs-dependent cyclic AMP accumulation. However, A2BAR G protein-coupling to other signaling events, e.g. ERK1/2 and calcium, is not well documented. We explored Gi, Gq/11 and Gs coupling in 1321 N1 astrocytoma, HEK293, and T24 bladder cancer cells endogenously expressing human A2BAR, using NECA or nonnucleoside BAY60-6583 as agonist, selective Gi, Gs and Gq/11 blockers, and CRISPR/Cas9-based Gq- and Gs-null HEK293 cells. In HEK293 cells, A2BAR… CONTINUE READING
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