Novel non-xanthine antagonist of the A2B adenosine receptor: From HTS hit to lead structure.
Sign Up to like & getrecommendations! Published in 2019 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2018.11.045
Abstract: The A2B adenosine receptor is a G protein-coupled receptor that belongs to the four member family of adenosine receptors: A1, A2A, A2B, A3. While adenosine-mediated A2B receptor signaling attenuates acute inflammation, facilitates tissue adaptation to… read more here.
Keywords: a2b receptor; adenosine receptor; a2b adenosine; structure ... See more keywords
Exploring the Effect of Halogenation in a Series of Potent and Selective A2B Adenosine Receptor Antagonists
Sign Up to like & getrecommendations! Published in 2022 at "Journal of Medicinal Chemistry"
DOI: 10.1021/acs.jmedchem.2c01768
Abstract: The modulation of the A2B adenosine receptor is a promising strategy in cancer (immuno) therapy, with A2BAR antagonists emerging as immune checkpoint inhibitors. Herein, we report a systematic assessment of the impact of (di- and… read more here.
Keywords: affinity; halogenation; a2bar; a2b adenosine ... See more keywords
The A2B adenosine receptor in MDA-MB-231 breast cancer cells diminishes ERK1/2 phosphorylation by activation of MAPK-phosphatase-1
Sign Up to like & getrecommendations! Published in 2018 at "PLoS ONE"
DOI: 10.1371/journal.pone.0202914
Abstract: It was previously shown that the estrogen-receptor negative breast cancer cell line MBA-MD-231 expresses high levels of A2B adenosine receptors as the sole adenosine receptor subtype. These receptors couple to both, stimulation of adenylyl cyclase… read more here.
Keywords: erk1 phosphorylation; breast cancer; adenosine receptors; a2b adenosine ... See more keywords
A2B Adenosine Receptors and Sphingosine 1-Phosphate Signaling Cross-Talk in Oligodendrogliogenesis
Sign Up to like & getrecommendations! Published in 2021 at "Frontiers in Neuroscience"
DOI: 10.3389/fnins.2021.677988
Abstract: Oligodendrocyte-formed myelin sheaths allow fast synaptic transmission in the brain. Impairments in the process of myelination, or demyelinating insults, might cause chronic diseases such as multiple sclerosis (MS). Under physiological conditions, remyelination is an ongoing… read more here.
Keywords: sphingosine phosphate; a2b adenosine; adenosine receptors; phosphate signaling ... See more keywords
A2B Adenosine Receptor Enhances Chemoresistance of Glioblastoma Stem-Like Cells under Hypoxia: New Insights into MRP3 Transporter Function
Sign Up to like & getrecommendations! Published in 2022 at "International Journal of Molecular Sciences"
DOI: 10.3390/ijms23169022
Abstract: Glioblastoma is the most common and aggressive primary brain tumor, characterized by its high chemoresistance and the presence of a cell subpopulation that persists under hypoxic niches, called glioblastoma stem-like cells (GSCs). The chemoresistance of… read more here.
Keywords: glioblastoma stem; a2b adenosine; adenosine receptor; receptor ... See more keywords
A2B Adenosine Receptor in Idiopathic Pulmonary Fibrosis: Pursuing Proper Pit Stop to Interfere with Disease Progression
Sign Up to like & getrecommendations! Published in 2023 at "International Journal of Molecular Sciences"
DOI: 10.3390/ijms24054428
Abstract: Purine nucleotides and nucleosides are involved in various human physiological and pathological mechanisms. The pathological deregulation of purinergic signaling contributes to various chronic respiratory diseases. Among the adenosine receptors, A2B has the lowest affinity such… read more here.
Keywords: receptor idiopathic; progression; pulmonary fibrosis; a2b adenosine ... See more keywords