G protein-coupled receptors (GPCRs): advances in structures, mechanisms and drug discovery

M Zhang, T Chen, X Lu, X Lan, Z Chen… - Signal Transduction and …, 2024 - nature.com
G protein-coupled receptors (GPCRs), the largest family of human membrane proteins and
an important class of drug targets, play a role in maintaining numerous physiological …

[HTML][HTML] Presynaptic adenosine receptor heteromers as key modulators of glutamatergic and dopaminergic neurotransmission in the striatum

S Ferré, LI Sarasola, C Quiroz, F Ciruela - Neuropharmacology, 2023 - Elsevier
Adenosine plays a very significant role in modulating striatal glutamatergic and
dopaminergic neurotransmission. In the present essay we first review the extensive …

New paradigms in purinergic receptor ligand discovery

KA Jacobson, B Pradhan, Z Wen, A Pramanik - Neuropharmacology, 2023 - Elsevier
The discovery and clinical implementation of modulators of adenosine, P2Y and P2X
receptors (comprising nineteen subtypes) have progressed dramatically in∼ 50 years since …

[HTML][HTML] Homodimerization of CB2 cannabinoid receptor triggered by a bivalent ligand enhances cellular signaling

G Navarro, M Gómez-Autet, P Morales… - Pharmacological …, 2024 - Elsevier
G protein-coupled receptors (GPCRs) exist within a landscape of interconvertible
conformational states and in dynamic equilibrium between monomers and higher-order …

The crosstalk between 5-HT2AR and mGluR2 in schizophrenia

S Saha, J González-Maeso - Neuropharmacology, 2023 - Elsevier
Schizophrenia is a severe brain disorder that usually produces a lifetime of disability. First
generation or typical antipsychotics such as haloperidol and second generation or atypical …

Adenosine receptor signalling in Alzheimer's disease

PNH Trinh, JA Baltos, SD Hellyer, LT May… - Purinergic …, 2022 - Springer
Alzheimer's disease (AD) is the most common dementia in the elderly and its increasing
prevalence presents treatment challenges. Despite a better understanding of the disease …

Functional dynamics of G protein-coupled receptors reveal new routes for drug discovery

P Conflitti, E Lyman, MSP Sansom… - Nature Reviews Drug …, 2025 - nature.com
G protein-coupled receptors (GPCRs) are the largest human membrane protein family that
transduce extracellular signals into cellular responses. They are major pharmacological …

Optical control of dopamine D2-like receptors with cell-specific fast-relaxing photoswitches

BE Hetzler, P Donthamsetti, Z Peitsinis… - Journal of the …, 2023 - ACS Publications
Dopamine D2-like receptors (D2R, D3R, and D4R) control diverse physiological and
behavioral functions and are important targets for the treatment of a variety of …

[HTML][HTML] Overview of the role of purinergic signaling and insights into its role in cancer therapy

F Di Virgilio, V Vultaggio-Poma, M Tarantini… - Pharmacology & …, 2024 - Elsevier
Innovation of cancer therapy has received a dramatic acceleration over the last fifteen years
thanks to the introduction of the novel immune checkpoint inhibitors (ICI). On the other hand …

A Single Point Mutation Blocks the Entrance of Ligands to the Cannabinoid CB2 Receptor via the Lipid Bilayer

N Casajuana-Martin, G Navarro… - Journal of Chemical …, 2022 - ACS Publications
Molecular dynamic (MD) simulations have become a common tool to study the pathway of
ligand entry to the orthosteric binding site of G protein-coupled receptors. Here, we have …