International union of basic and clinical pharmacology. CXII: adenosine receptors: a further update
AP IJzerman, KA Jacobson, CE Müller… - Pharmacological …, 2022 - Elsevier
Abstract 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 …
Allosteric modulation of GPCRs: From structural insights to in silico drug discovery
M Persechino, JB Hedderich, P Kolb… - Pharmacology & …, 2022 - Elsevier
G protein-coupled receptors (GPCRs) play critical roles in human physiology and are one of
the prime targets for marketed drugs. While traditional drug discovery programs have …
the prime targets for marketed drugs. While traditional drug discovery programs have …
Human Adenosine A2A Receptor: Molecular Mechanism of Ligand Binding and Activation
B Carpenter, G Lebon - Frontiers in pharmacology, 2017 - frontiersin.org
Adenosine receptors (ARs) comprise the P1 class of purinergic receptors and belong to the
largest family of integral membrane proteins in the human genome, the G protein-coupled …
largest family of integral membrane proteins in the human genome, the G protein-coupled …
Royal jelly alleviates cognitive deficits and β-amyloid accumulation in APP/PS1 mouse model via activation of the cAMP/PKA/CREB/BDNF pathway and inhibition of …
M You, Y Pan, Y Liu, Y Chen, Y Wu, J Si… - Frontiers in Aging …, 2019 - frontiersin.org
Alzheimer's disease (AD) is characterized clinically by progressive cognitive decline and
pathologically by the accumulation of amyloid-β (Aβ) in the brain. Royal jelly (RJ), a …
pathologically by the accumulation of amyloid-β (Aβ) in the brain. Royal jelly (RJ), a …
Balancing G protein selectivity and efficacy in the adenosine A2A receptor
The adenosine A2A receptor (A2AR) engages several G proteins, notably Go and its
cognate Gs protein. This coupling promiscuity is facilitated by a dynamic ensemble, revealed …
cognate Gs protein. This coupling promiscuity is facilitated by a dynamic ensemble, revealed …
[HTML][HTML] Minute-timescale free-energy calculations reveal a pseudo-active state in the adenosine A2A receptor activation mechanism
G protein-coupled receptors (GPCRs) are membrane proteins targeted by over one-third of
marketed drugs. Understanding their activation mechanism is essential for precise …
marketed drugs. Understanding their activation mechanism is essential for precise …
G protein-coupled receptor (GPCR) reconstitution and labeling for solution nuclear magnetic resonance (NMR) studies of the structural basis of transmembrane …
G protein-coupled receptors (GPCRs) are a large membrane protein family found in higher
organisms, including the human body. GPCRs mediate cellular responses to diverse …
organisms, including the human body. GPCRs mediate cellular responses to diverse …
Homo-oligomerization of the human adenosine A2A receptor is driven by the intrinsically disordered C-terminus
G protein-coupled receptors (GPCRs) have long been shown to exist as oligomers with
functional properties distinct from those of the monomeric counterparts, but the driving …
functional properties distinct from those of the monomeric counterparts, but the driving …
Insights into adenosine A2A receptor activation through cooperative modulation of agonist and allosteric lipid interactions
A Bruzzese, JAR Dalton, J Giraldo - PLoS computational biology, 2020 - journals.plos.org
The activation process of G protein-coupled receptors (GPCRs) has been extensively
studied, both experimentally and computationally. In particular, Molecular Dynamics (MD) …
studied, both experimentally and computationally. In particular, Molecular Dynamics (MD) …
Quantitative structural assessment of graded receptor agonism
Ligand–receptor interactions, which are ubiquitous in physiology, are described by
theoretical models of receptor pharmacology. Structural evidence for graded efficacy …
theoretical models of receptor pharmacology. Structural evidence for graded efficacy …