Results 11 to 20 of about 23,527,897 (360)
Cryo-EM structure of the adenosine A2A receptor coupled to an engineered heterotrimeric G protein
eLife, 2018 The adenosine A2A receptor (A2AR) is a prototypical G protein-coupled receptor (GPCR) that couples to the heterotrimeric G protein GS. Here, we determine the structure by electron cryo-microscopy (cryo-EM) of A2AR at pH 7.5 bound to the small molecule ...
Javier García-Nafría +4 more
doaj +2 more sources
Ligand and G-protein selectivity in the κ-opioid receptor
Nature, 2023 The κ-opioid receptor (KOR) represents a highly desirable therapeutic target for treating not only pain but also addiction and affective disorders^ 1 .
Jianming Han +13 more
semanticscholar +1 more source
THE CONCISE GUIDE TO PHARMACOLOGY 2021/22: G protein‐coupled receptors
British Journal of Pharmacology, 2021 The Concise Guide to PHARMACOLOGY 2021/22 is the fifth in this series of biennial publications. The Concise Guide provides concise overviews, mostly in tabular format, of the key properties of nearly 1900 human drug targets with an emphasis on selective ...
Stephen P. H. Alexander +154 more
semanticscholar +1 more source
G protein-coupled receptors: structure- and function-based drug discovery
Signal Transduction and Targeted Therapy, 2021 As one of the most successful therapeutic target families, G protein-coupled receptors (GPCRs) have experienced a transformation from random ligand screening to knowledge-driven drug design.
Dehua Yang +14 more
semanticscholar +1 more source
Molecular mechanism of biased signaling in a prototypical G protein–coupled receptor
Science, 2020 Choosing the drug to fit the protein Many approved drugs bind to G protein–coupled receptors (GPCRs). A challenge in targeting GPCRs is that different ligands preferentially activate different signaling pathways.
Carl-Mikael Suomivuori +10 more
semanticscholar +1 more source
Gi- and Gs-coupled GPCRs show different modes of G-protein binding. [PDF]
, 2018 More than two decades ago, the activation mechanism for the membrane-bound photoreceptor and prototypical G protein-coupled receptor (GPCR) rhodopsin was uncovered.
Altenbach, Christian +7 more
core +1 more source
G Protein‐Coupled receptors and heterotrimeric G proteins as cancer drivers
FEBS Letters, 2020 G protein‐coupled receptors (GPCRs) and heterotrimeric G proteins play central roles in a diverse array of cellular processes. As such, dysregulation of GPCRs and their coupled heterotrimeric G proteins can dramatically alter the signalling landscape and
Nadia Arang, J. Gutkind
semanticscholar +1 more source
mSystems, 2019 The release of synthetic chemical pollutants in the environment is posing serious health risks. Enzymes, including oxygenases, play a crucial role in xenobiotic degradation. In the present study, we employed a functional metagenomics approach to overcome
Chandni Sidhu +3 more
doaj +3 more sources
G protein-coupled receptor-G protein interactions: a single-molecule perspective.
Physiological Reviews, 2020 G protein-coupled receptors (GPCRs) regulate many cellular and physiological processes, responding to a diverse range of extracellular stimuli including hormones, neurotransmitters, odorants and light.
D. Calebiro +4 more
semanticscholar +1 more source
Vaccines, 2019 Human metapneumovirus (HMPV) is a major pediatric respiratory pathogen with currently no specific treatment or licensed vaccine. Different strategies to prevent this infection have been evaluated, including live-attenuated vaccines (LAV) based on SH and ...
Julia Dubois +16 more
doaj +1 more source