Elsevier

Life Sciences

Volume 62, Issues 17–18, 27 March 1998, Pages 1519-1524
Life Sciences

The structure and function of A1 and A2B adenosine receptors

https://doi.org/10.1016/S0024-3205(98)00100-3Get rights and content

Abstract

Of the four G protein coupled adenosine receptor (AR) subtypes, the A1 is best suited for studies of reconstitution with G proteins. Recombinant A1 receptors extended with hexahistidine and FLAG have been purified to near homogeneity. In reconstitution assays using pure recombinant G protein subunits, the composition of the γ subunit influences coupling to purified A1ARs. The least well characterized AR is the A2B. New data indicate that A2BARs can trigger the degranulation of canine and human mast cell lines. Recombinant human A2BARs are blocked by the anti-asthma drugs theophylline and enprofylline at concentrations that are used therapeutically to treat asthma. Although A2BARs have long been known to stimulate adenylyl cyclase, they also can activate phospholipase C and mobilize Ca2+ by signaling through Gq/11. There is great potential for new therapies based on compounds that selectively target individual AR subtypes.

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