Faculty Collaboration Database

The structure and function of A1 and A2B adenosine receptors. Life Sci 1998;62(17-18):1519-24

Date

05/19/1998

Pubmed ID

9585129

DOI

10.1016/s0024-3205(98)00100-3

Scopus ID

2-s2.0-0032571017 (requires institutional sign-in at Scopus site)   45 Citations

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 gamma subunit influences coupling to purified A1ARs. The least well characterized AR is the A2B. New data indicate that A(2B)ARs can trigger the degranulation of canine and human mast cell lines. Recombinant human A(2B)ARs are blocked by the anti-asthma drugs theophylline and enprofylline at concentrations that are used therapeutically to treat asthma. Although A(2B)ARs 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.

Author List

Linden J, Auchampach JA, Jin X, Figler RA

Author

John A. Auchampach PhD Professor in the Pharmacology and Toxicology department at Medical College of Wisconsin

MESH terms used to index this publication - Major topics in bold

Animals
Baculoviridae
COS Cells
Cattle
Dogs
GTP-Binding Proteins
Histidine
Humans
Receptors, Purinergic P1
Recombinant Proteins
Spodoptera
Structure-Activity Relationship