International union of basic and clinical pharmacology. CXII: adenosine receptors: a further update
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 …
Membranes under the magnetic lens: a dive into the diverse world of membrane protein structures using Cryo-EM
Membrane proteins are highly diverse in both structure and function and can, therefore,
present different challenges for structure determination. They are biologically important for …
present different challenges for structure determination. They are biologically important for …
GPCR activation and GRK2 assembly by a biased intracellular agonist
J Duan, H Liu, F Zhao, Q Yuan, Y Ji, X Cai, X He, X Li… - Nature, 2023 - nature.com
Phosphorylation of G-protein-coupled receptors (GPCRs) by GPCR kinases (GRKs)
desensitizes G-protein signalling and promotes arrestin signalling, which is also modulated …
desensitizes G-protein signalling and promotes arrestin signalling, which is also modulated …
A µ-opioid receptor modulator that works cooperatively with naloxone
The µ-opioid receptor (µOR) is a well-established target for analgesia, yet conventional
opioid receptor agonists cause serious adverse effects, notably addiction and respiratory …
opioid receptor agonists cause serious adverse effects, notably addiction and respiratory …
Biased allosteric activation of ketone body receptor HCAR2 suppresses inflammation
C Zhao, H Wang, Y Liu, L Cheng, B Wang, X Tian, H Fu… - Molecular Cell, 2023 - cell.com
Summary Hydroxycarboxylic acid receptor 2 (HCAR2), modulated by endogenous ketone
body β-hydroxybutyrate and exogenous niacin, is a promising therapeutic target for …
body β-hydroxybutyrate and exogenous niacin, is a promising therapeutic target for …
State-specific protein–ligand complex structure prediction with a multiscale deep generative model
The binding complexes formed by proteins and small molecule ligands are ubiquitous and
critical to life. Despite recent advancements in protein structure prediction, existing …
critical to life. Despite recent advancements in protein structure prediction, existing …
Cryo-EM structure of the human adenosine A2B receptor–Gs signaling complex
The human adenosine A2B receptor (A2BR) is a class AG protein–coupled receptor that is
involved in several major physiological and pathological processes throughout the body …
involved in several major physiological and pathological processes throughout the body …
Positive allosteric modulation of a GPCR ternary complex
The activation of a G protein–coupled receptor (GPCR) leads to the formation of a ternary
complex between agonist, receptor, and G protein that is characterized by high-affinity …
complex between agonist, receptor, and G protein that is characterized by high-affinity …
Pharmacology of adenosine receptors: Recent advancements
Adenosine receptors (ARs) are widely acknowledged pharmacological targets yet are still
underutilized in clinical practice. Their ubiquitous distribution in almost all cells and tissues …
underutilized in clinical practice. Their ubiquitous distribution in almost all cells and tissues …
[HTML][HTML] Delineating the activation mechanism and conformational landscape of a class BG protein-coupled receptor glucagon receptor
Y Wang, M Li, W Liang, X Shi, J Fan, R Kong… - Computational and …, 2022 - Elsevier
Class BG protein-coupled receptors (GPCRs) are important targets in the treatment of
metabolic syndrome and diabetes. Although multiple structures of class B GPCRs–G protein …
metabolic syndrome and diabetes. Although multiple structures of class B GPCRs–G protein …