Abstract
The adenosine A2B receptor (A2BAR) is one of four adenosine receptor subtypes belonging to the Class A family of G protein-coupled receptors (GPCRs). Until recently, the A2BAR remained poorly characterised, in part due to its relatively low affinity for the endogenous agonist adenosine and therefore presumed minor physiological significance. However, the substantial increase in extracellular adenosine concentration, the sensitisation of the receptor and the upregulation of A2BAR expression under conditions of hypoxia and inflammation, suggest the A2BAR as an exciting therapeutic target in a variety of pathological disease states. Here we discuss the pharmacology of the A2BAR and outline its role in pathophysiology including ischaemia-reperfusion injury, fibrosis, inflammation and cancer.
| Original language | English |
|---|---|
| Pages (from-to) | 20-33 |
| Number of pages | 14 |
| Journal | Pharmacology and Therapeutics |
| Volume | 198 |
| DOIs | |
| Publication status | Published - 1 Jan 2019 |
Keywords
- adenosine A receptor
- cancer
- fibrosis
- inflammation and immune response
- ischaemia-reperfusion injury
Cite this
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The adenosine A 2B G protein-coupled receptor : Recent advances and therapeutic implications. / Vecchio, Elizabeth A.; White, Paul J.; May, Lauren T.
In: Pharmacology and Therapeutics, Vol. 198, 01.01.2019, p. 20-33.Research output: Contribution to journal › Review Article › Research › peer-review
TY - JOUR
T1 - The adenosine A 2B G protein-coupled receptor
T2 - Recent advances and therapeutic implications
AU - Vecchio, Elizabeth A.
AU - White, Paul J.
AU - May, Lauren T.
PY - 2019/1/1
Y1 - 2019/1/1
N2 - The adenosine A2B receptor (A2BAR) is one of four adenosine receptor subtypes belonging to the Class A family of G protein-coupled receptors (GPCRs). Until recently, the A2BAR remained poorly characterised, in part due to its relatively low affinity for the endogenous agonist adenosine and therefore presumed minor physiological significance. However, the substantial increase in extracellular adenosine concentration, the sensitisation of the receptor and the upregulation of A2BAR expression under conditions of hypoxia and inflammation, suggest the A2BAR as an exciting therapeutic target in a variety of pathological disease states. Here we discuss the pharmacology of the A2BAR and outline its role in pathophysiology including ischaemia-reperfusion injury, fibrosis, inflammation and cancer.
AB - The adenosine A2B receptor (A2BAR) is one of four adenosine receptor subtypes belonging to the Class A family of G protein-coupled receptors (GPCRs). Until recently, the A2BAR remained poorly characterised, in part due to its relatively low affinity for the endogenous agonist adenosine and therefore presumed minor physiological significance. However, the substantial increase in extracellular adenosine concentration, the sensitisation of the receptor and the upregulation of A2BAR expression under conditions of hypoxia and inflammation, suggest the A2BAR as an exciting therapeutic target in a variety of pathological disease states. Here we discuss the pharmacology of the A2BAR and outline its role in pathophysiology including ischaemia-reperfusion injury, fibrosis, inflammation and cancer.
KW - adenosine A receptor
KW - cancer
KW - fibrosis
KW - inflammation and immune response
KW - ischaemia-reperfusion injury
UR - http://www.scopus.com/inward/record.url?scp=85061894811&partnerID=8YFLogxK
U2 - 10.1016/j.pharmthera.2019.01.003
DO - 10.1016/j.pharmthera.2019.01.003
M3 - Review Article
VL - 198
SP - 20
EP - 33
JO - Pharmacology and Therapeutics
JF - Pharmacology and Therapeutics
SN - 0163-7258
ER -