Pharmacology of adenosine receptors: the state of the art
Adenosine is a ubiquitous endogenous autacoid whose effects are triggered through the
enrollment of four G protein-coupled receptors: A1, A2A, A2B, and A3. Due to the rapid …
enrollment of four G protein-coupled receptors: A1, A2A, A2B, and A3. Due to the rapid …
Targeting immunosuppressive adenosine in cancer
Despite the success of anti-programmed cell death protein 1 (PD1), anti-PD1 ligand 1
(PDL1) and anti-cytotoxic T lymphocyte antigen 4 (CTLA4) therapies in advanced cancer, a …
(PDL1) and anti-cytotoxic T lymphocyte antigen 4 (CTLA4) therapies in advanced cancer, a …
[HTML][HTML] Targeting adenosine in cancer immunotherapy to enhance T-cell function
S Vigano, D Alatzoglou, M Irving… - Frontiers in …, 2019 - frontiersin.org
T cells play a critical role in cancer control, but a range of potent immunosuppressive
mechanisms can be upregulated in the tumor microenvironment (TME) to abrogate their …
mechanisms can be upregulated in the tumor microenvironment (TME) to abrogate their …
Adenosine 2A receptor blockade as an immunotherapy for treatment-refractory renal cell cancer
L Fong, A Hotson, JD Powderly, M Sznol, RS Heist… - Cancer discovery, 2020 - AACR
Adenosine mediates immunosuppression within the tumor microenvironment through
triggering adenosine 2A receptors (A2AR) on immune cells. To determine whether this …
triggering adenosine 2A receptors (A2AR) on immune cells. To determine whether this …
[HTML][HTML] Protein–ligand binding with the coarse-grained Martini model
The detailed understanding of the binding of small molecules to proteins is the key for the
development of novel drugs or to increase the acceptance of substrates by enzymes …
development of novel drugs or to increase the acceptance of substrates by enzymes …
[HTML][HTML] Purinergic signalling: therapeutic developments
G Burnstock - Frontiers in pharmacology, 2017 - frontiersin.org
Purinergic signalling, ie, the role of nucleotides as extracellular signalling molecules, was
proposed in 1972. However, this concept was not well accepted until the early 1990's when …
proposed in 1972. However, this concept was not well accepted until the early 1990's when …
[HTML][HTML] Delineating the conformational landscape of the adenosine A2A receptor during G protein coupling
G-protein-coupled receptors (GPCRs) represent a ubiquitous membrane protein family and
are important drug targets. Their diverse signaling pathways are driven by complex …
are important drug targets. Their diverse signaling pathways are driven by complex …
Comparative studies of AlphaFold, RoseTTAFold and Modeller: a case study involving the use of G-protein-coupled receptors
Neural network (NN)-based protein modeling methods have improved significantly in recent
years. Although the overall accuracy of the two non-homology-based modeling methods …
years. Although the overall accuracy of the two non-homology-based modeling methods …
The medicinal chemistry of caffeine
G Faudone, S Arifi, D Merk - Journal of medicinal chemistry, 2021 - ACS Publications
The purine alkaloid caffeine is the most widely consumed psychostimulant drug in the world
and has multiple beneficial pharmacological activities, for example, in neurodegenerative …
and has multiple beneficial pharmacological activities, for example, in neurodegenerative …
[HTML][HTML] Cryo-EM structure of the adenosine A2A receptor coupled to an engineered heterotrimeric G protein
The adenosine A2A receptor (A2AR) is a prototypical G protein-coupled receptor (GPCR)
that couples to the heterotrimeric G protein GS. Here, we determine the structure by electron …
that couples to the heterotrimeric G protein GS. Here, we determine the structure by electron …