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 …
[HTML][HTML] 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 …
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 …
[HTML][HTML] 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 …
Anxiety and dysautonomia symptoms in patients with a NaV1.7 mutation and the potential benefits of low-dose short-acting guanfacine
R de Cássia Collaço, M Lammens, C Blevins… - Clinical Autonomic …, 2024 - Springer
Purpose Guanfacine is an α2A-adrenergic receptor agonist, FDA-approved to treat attention-
deficit hyperactivity disorder and high blood pressure, typically as an extended-release …
deficit hyperactivity disorder and high blood pressure, typically as an extended-release …
Identification of a Novel Subtype-Selective α1B-Adrenoceptor Antagonist
A Abdul-Ridha, LA de Zhang, AH Betrie… - ACS Chemical …, 2024 - ACS Publications
α1A-, α1B-, and α1D-adrenoceptors (α1-ARs) are members of the adrenoceptor G protein-
coupled receptor family that are activated by adrenaline (epinephrine) and noradrenaline …
coupled receptor family that are activated by adrenaline (epinephrine) and noradrenaline …