International union of basic and clinical pharmacology. CXII: adenosine receptors: a further update
AP IJzerman, KA Jacobson, CE Müller… - Pharmacological …, 2022 - ASPET
Our previous International Union of Basic and Clinical Pharmacology report on the
nomenclature and classification of adenosine receptors (2011) contained a number of …
nomenclature and classification of adenosine receptors (2011) contained a number of …
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 …
[HTML][HTML] Common activation mechanism of class A GPCRs
Class A G-protein-coupled receptors (GPCRs) influence virtually every aspect of human
physiology. Understanding receptor activation mechanism is critical for discovering novel …
physiology. Understanding receptor activation mechanism is critical for discovering novel …
[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 …
GPCR drug discovery: integrating solution NMR data with crystal and cryo-EM structures
I Shimada, T Ueda, Y Kofuku, MT Eddy… - Nature Reviews Drug …, 2019 - nature.com
The 826 G protein-coupled receptors (GPCRs) in the human proteome regulate key
physiological processes and thus have long been attractive drug targets. With the crystal …
physiological processes and thus have long been attractive drug targets. With the crystal …
[HTML][HTML] Anionic phospholipids control mechanisms of GPCR-G protein recognition
G protein-coupled receptors (GPCRs) are embedded in phospholipids that strongly
influence drug-stimulated signaling. Anionic lipids are particularly important for GPCR …
influence drug-stimulated signaling. Anionic lipids are particularly important for GPCR …
[HTML][HTML] Historical and current adenosine receptor agonists in preclinical and clinical development
KA Jacobson, DK Tosh, S Jain, ZG Gao - Frontiers in cellular …, 2019 - frontiersin.org
Adenosine receptors (ARs) function in the body's response to conditions of pathology and
stress associated with a functional imbalance, such as in the supply and demand of …
stress associated with a functional imbalance, such as in the supply and demand of …
The role of structural dynamics in GPCR‐mediated signaling
D Hilger - The FEBS journal, 2021 - Wiley Online Library
G protein‐coupled receptors (GPCRs) play critical roles in the regulation of human
physiology in response to a wide array of different extracellular stimuli and thus represent …
physiology in response to a wide array of different extracellular stimuli and thus represent …
Lipid nanodiscs for high-resolution NMR studies of membrane proteins
Membrane proteins (MPs) play essential roles in numerous cellular processes. Because
around 70% of the currently marketed drugs target MPs, a detailed understanding of their …
around 70% of the currently marketed drugs target MPs, a detailed understanding of their …
[HTML][HTML] Structural connection between activation microswitch and allosteric sodium site in GPCR signaling
Sodium ions are endogenous allosteric modulators of many G-protein-coupled receptors
(GPCRs). Mutation of key residues in the sodium binding motif causes a striking effect on G …
(GPCRs). Mutation of key residues in the sodium binding motif causes a striking effect on G …