Structure-based discovery of nonopioid analgesics acting through the α2A-adrenergic receptor
Because nonopioid analgesics are much sought after, we computationally docked more
than 301 million virtual molecules against a validated pain target, the α2A-adrenergic …
than 301 million virtual molecules against a validated pain target, the α2A-adrenergic …
Adrenoceptor Desensitization: Current understanding of mechanisms
D Maaliki, AA Jaffa, S Nasser, A Sahebkar… - Pharmacological …, 2024 - ASPET
G-protein coupled receptors (GPCRs) transduce a wide range of extracellular signals. They
are key players in the majority of biologic functions including vision, olfaction, chemotaxis …
are key players in the majority of biologic functions including vision, olfaction, chemotaxis …
Structural basis of α1A-adrenergic receptor activation and recognition by an extracellular nanobody
Y Toyoda, A Zhu, F Kong, S Shan, J Zhao… - Nature …, 2023 - nature.com
The α1A-adrenergic receptor (α1AAR) belongs to the family of G protein-coupled receptors
that respond to adrenaline and noradrenaline. α1AAR is involved in smooth muscle …
that respond to adrenaline and noradrenaline. α1AAR is involved in smooth muscle …
A novel “activation switch” motif common to all aminergic receptors
Aminergic receptors are G protein-coupled receptors (GPCRs) that transduce signals from
small endogenous biogenic amines to regulate intracellular signaling pathways. Agonist …
small endogenous biogenic amines to regulate intracellular signaling pathways. Agonist …
Therapeutic antagonism of the neurokinin 1 receptor in endosomes provides sustained pain relief
The hypothesis that sustained G protein-coupled receptor (GPCR) signaling from
endosomes mediates pain is based on studies with endocytosis inhibitors and lipid …
endosomes mediates pain is based on studies with endocytosis inhibitors and lipid …
Structural basis of psychedelic LSD recognition at dopamine D1 receptor
Understanding the kinetics of LSD in receptors and subsequent induced signaling is crucial
for comprehending both the psychoactive and therapeutic effects of LSD. Despite extensive …
for comprehending both the psychoactive and therapeutic effects of LSD. Despite extensive …
Distinct binding conformations of epinephrine with α-and β-adrenergic receptors
Agonists targeting α2-adrenergic receptors (ARs) are used to treat diverse conditions,
including hypertension, attention-deficit/hyperactivity disorder, pain, panic disorders, opioid …
including hypertension, attention-deficit/hyperactivity disorder, pain, panic disorders, opioid …
Segregation of nascent GPCRs in the ER-to-Golgi transport by CCHCR1 via direct interaction
X Xu, L Qiu, M Zhang, G Wu - Journal of Cell Science, 2024 - journals.biologists.com
ABSTRACT G protein-coupled receptors (GPCRs) constitute the largest superfamily of cell
surface signaling proteins that share a common structural topology. When compared with …
surface signaling proteins that share a common structural topology. When compared with …
Novel Scaffold Agonists of the α2A Adrenergic Receptor Identified via Ensemble-Based Strategy
S Sun, P Li, J Wang, D Zhao, T Yang, P Zhou, R Su… - Molecules, 2024 - mdpi.com
The α2A adrenergic receptor (α2A-AR) serves as a critical molecular target for sedatives and
analgesics. However, α2A-AR ligands with an imidazole ring also interact with an …
analgesics. However, α2A-AR ligands with an imidazole ring also interact with an …
Designing Chromane Derivatives as α2A-Adrenoceptor Selective Agonists via Conformation Constraint
X Lv, P Zhou, X Qiao, Y Li, X Yang… - Journal of Medicinal …, 2024 - ACS Publications
Enhancing the selectivity of alpha2-adrenoceptor (α2A-AR) agonists remains an unresolved
issue. Herein, we reported the design of an α2A-AR agonist using the conformation …
issue. Herein, we reported the design of an α2A-AR agonist using the conformation …