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 …
Structure-based virtual screening for ligands of G protein–coupled receptors: what can molecular docking do for you?
F Ballante, AJ Kooistra, S Kampen, C de Graaf… - Pharmacological …, 2021 - ASPET
G protein–coupled receptors (GPCRs) constitute the largest family of membrane proteins in
the human genome and are important therapeutic targets. During the last decade, the …
the human genome and are important therapeutic targets. During the last decade, the …
[HTML][HTML] Structure of a hallucinogen-activated Gq-coupled 5-HT2A serotonin receptor
Hallucinogens like lysergic acid diethylamide (LSD), psilocybin, and substituted N-benzyl
phenylalkylamines are widely used recreationally with psilocybin being considered as a …
phenylalkylamines are widely used recreationally with psilocybin being considered as a …
Structure, function and pharmacology of human itch GPCRs
The MRGPRX family of receptors (MRGPRX1–4) is a family of mas-related G-protein-
coupled receptors that have evolved relatively recently. Of these, MRGPRX2 and MRGPRX4 …
coupled receptors that have evolved relatively recently. Of these, MRGPRX2 and MRGPRX4 …
GPCR activation mechanisms across classes and macro/microscales
Two-thirds of human hormones and one-third of clinical drugs activate~ 350 G-protein-
coupled receptors (GPCR) belonging to four classes: A, B1, C and F. Whereas a model of …
coupled receptors (GPCR) belonging to four classes: A, B1, C and F. Whereas a model of …
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 …
Positive allosteric mechanisms of adenosine A1 receptor-mediated analgesia
The adenosine A1 receptor (A1R) is a promising therapeutic target for non-opioid analgesic
agents to treat neuropathic pain,. However, development of analgesic orthosteric A1R …
agents to treat neuropathic pain,. However, development of analgesic orthosteric A1R …
Gaussian accelerated molecular dynamics: Principles and applications
Gaussian accelerated molecular dynamics (GaMD) is a robust computational method for
simultaneous unconstrained enhanced sampling and free energy calculations of …
simultaneous unconstrained enhanced sampling and free energy calculations of …
[HTML][HTML] Illuminating G-protein-coupling selectivity of GPCRs
Heterotrimetic G proteins consist of four subfamilies (G s, G i/o, G q/11, and G 12/13) that
mediate signaling via G-protein-coupled receptors (GPCRs), principally by receptors binding …
mediate signaling via G-protein-coupled receptors (GPCRs), principally by receptors binding …
Activation and signaling mechanism revealed by cannabinoid receptor-Gi complex structures
T Hua, X Li, L Wu, C Iliopoulos-Tsoutsouvas, Y Wang… - Cell, 2020 - cell.com
Human endocannabinoid systems modulate multiple physiological processes mainly
through the activation of cannabinoid receptors CB1 and CB2. Their high sequence …
through the activation of cannabinoid receptors CB1 and CB2. Their high sequence …