International union of basic and clinical pharmacology. CXII: adenosine receptors: a further update

AP IJzerman, KA Jacobson, CE Müller… - Pharmacological …, 2022 - Elsevier
Abstract Our previous International Union of Basic and Clinical Pharmacology report on the
nomenclature and classification of adenosine receptors (2011) contained a number of …

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] 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 …

Allosterism in the adenosine A2A and cannabinoid CB2 heteromer

C Llinas del Torrent, I Raïch, A Gonzalez… - British Journal of …, 2024 - Wiley Online Library
Abstract Background and Purpose Allosterism is a regulatory mechanism for GPCRs that
can be attained by ligand‐binding or protein–protein interactions with another GPCR. We …

Structure and function of adenosine receptor heteromers

R Franco, A Cordomí, C Llinas del Torrent… - Cellular and Molecular …, 2021 - Springer
Adenosine is one of the most ancient signaling molecules and has receptors in both animals
and plants. In mammals there are four specific receptors, A 1, A 2A, A 2B, and A 3, which …

Design of Negative and Positive Allosteric Modulators of the Cannabinoid CB2 Receptor Derived from the Natural Product Cannabidiol

G Navarro, A Gonzalez… - Journal of Medicinal …, 2021 - ACS Publications
Cannabidiol (CBD), the second most abundant of the active compounds found in the
Cannabis sativa plant, is of increasing interest because it is approved for human use and is …

[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 …

Unique pharmacodynamic properties and low abuse liability of the µ-opioid receptor ligand (S)-methadone

MR Levinstein, PA De Oliveira… - Molecular …, 2024 - nature.com
Abstract (R, S)-methadone ((R, S)-MTD) is a µ-opioid receptor (MOR) agonist comprised of
(R)-MTD and (S)-MTD enantiomers.(S)-MTD is being developed as an antidepressant and is …

The Leu/Val6.51 Side Chain of Cannabinoid Receptors Regulates the Binding Mode of the Alkyl Chain of Δ9-Tetrahydrocannabinol

C Llinas del Torrent, I Raïch, A Gonzalez… - Journal of Chemical …, 2023 - ACS Publications
(−)-Δ9-trans-tetrahydrocannabinol (THC), which is the principal psychoactive constituent of
Cannabis, mediates its action by binding to two members of the G-protein-coupled receptor …

[HTML][HTML] Minute-timescale free-energy calculations reveal a pseudo-active state in the adenosine A2A receptor activation mechanism

VM D'Amore, P Conflitti, L Marinelli, V Limongelli - Chem, 2024 - cell.com
G protein-coupled receptors (GPCRs) are membrane proteins targeted by over one-third of
marketed drugs. Understanding their activation mechanism is essential for precise …