Abstract
A2B adenosine receptors (A2BARs) are in the focus of interest as drug targets in (immuno)oncology since antagonists show anti-proliferative, anti-angiogenic, anti-metastatic, and immunostimulatory properties. Additional (poten-tial) indications for A2BAR antagonists include inflammatory (pulmonary, colon) and autoimmune diseases, pain, fibrosis, infectious diseases, diabetes, and more. Agonists were found to exhibit cardioprotective properties. The A2BAR is most closely related to the A2AAR subtype. Both are Gs protein-coupled receptors, but the A2BAR is additionally coupled to Gq proteins. A2BAR expression is upregulated under pathological conditions (hypoxia, inflammation, ischemia) and on many cancer cells. A2BARs form stable heteromeric complexes with A2AARs when co-expressed, and thereby completely block A2AAR signaling. There is still a lack of potent, selective, and fully efficacious A2BAR agonists, while structurally diverse potent and selective competitive antagonists for A2BARs have become available. The first positive and negative allosteric modulators for A2BARs were recently described. For the labeling of A2BARs, antagonist radioligands have been developed, and recently the first potent and selective fluorescent ligands were reported.
| Original language | English |
|---|---|
| Pages (from-to) | 137-168 |
| Number of pages | 32 |
| Journal | Receptors |
| Volume | 34 |
| DOIs | |
| Publication status | Published - Jan 1 2018 |
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Keywords
- A adenosine receptor
- Agonist
- Antagonist
- Cancer
- Inflammation
- Structure
ASJC Scopus subject areas
- Medicine(all)
Cite this
Medicinal chemistry of a2B adenosine receptors. / Müller, Christa E.; Baqi, Younis; Hinz, Sonja; Namasivayam, Vigneshwaran.
In: Receptors, Vol. 34, 01.01.2018, p. 137-168.Research output: Contribution to journal › Article
}
TY - JOUR
T1 - Medicinal chemistry of a2B adenosine receptors
AU - Müller, Christa E.
AU - Baqi, Younis
AU - Hinz, Sonja
AU - Namasivayam, Vigneshwaran
PY - 2018/1/1
Y1 - 2018/1/1
N2 - A2B adenosine receptors (A2BARs) are in the focus of interest as drug targets in (immuno)oncology since antagonists show anti-proliferative, anti-angiogenic, anti-metastatic, and immunostimulatory properties. Additional (poten-tial) indications for A2BAR antagonists include inflammatory (pulmonary, colon) and autoimmune diseases, pain, fibrosis, infectious diseases, diabetes, and more. Agonists were found to exhibit cardioprotective properties. The A2BAR is most closely related to the A2AAR subtype. Both are Gs protein-coupled receptors, but the A2BAR is additionally coupled to Gq proteins. A2BAR expression is upregulated under pathological conditions (hypoxia, inflammation, ischemia) and on many cancer cells. A2BARs form stable heteromeric complexes with A2AARs when co-expressed, and thereby completely block A2AAR signaling. There is still a lack of potent, selective, and fully efficacious A2BAR agonists, while structurally diverse potent and selective competitive antagonists for A2BARs have become available. The first positive and negative allosteric modulators for A2BARs were recently described. For the labeling of A2BARs, antagonist radioligands have been developed, and recently the first potent and selective fluorescent ligands were reported.
AB - A2B adenosine receptors (A2BARs) are in the focus of interest as drug targets in (immuno)oncology since antagonists show anti-proliferative, anti-angiogenic, anti-metastatic, and immunostimulatory properties. Additional (poten-tial) indications for A2BAR antagonists include inflammatory (pulmonary, colon) and autoimmune diseases, pain, fibrosis, infectious diseases, diabetes, and more. Agonists were found to exhibit cardioprotective properties. The A2BAR is most closely related to the A2AAR subtype. Both are Gs protein-coupled receptors, but the A2BAR is additionally coupled to Gq proteins. A2BAR expression is upregulated under pathological conditions (hypoxia, inflammation, ischemia) and on many cancer cells. A2BARs form stable heteromeric complexes with A2AARs when co-expressed, and thereby completely block A2AAR signaling. There is still a lack of potent, selective, and fully efficacious A2BAR agonists, while structurally diverse potent and selective competitive antagonists for A2BARs have become available. The first positive and negative allosteric modulators for A2BARs were recently described. For the labeling of A2BARs, antagonist radioligands have been developed, and recently the first potent and selective fluorescent ligands were reported.
KW - A adenosine receptor
KW - Agonist
KW - Antagonist
KW - Cancer
KW - Inflammation
KW - Structure
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UR - http://www.scopus.com/inward/citedby.url?scp=85052243403&partnerID=8YFLogxK
U2 - 10.1007/978-3-319-90808-3_6
DO - 10.1007/978-3-319-90808-3_6
M3 - Article
VL - 34
SP - 137
EP - 168
JO - Receptors
JF - Receptors
SN - 1048-6909
ER -