Exploring the Activation Mechanism of the GPR183 Receptor
The G protein-coupled receptors (GPCRs) play a pivotal role in numerous biological
processes as crucial cell membrane receptors. However, the dynamic mechanisms …
processes as crucial cell membrane receptors. However, the dynamic mechanisms …
Activation and signaling mechanism revealed by GPR119-Gs complex structures
Y Qian, J Wang, L Yang, Y Liu, L Wang, W Liu… - Nature …, 2022 - nature.com
Agonists selectively targeting cannabinoid receptor-like G-protein-coupled receptor (GPCR)
GPR119 hold promise for treating metabolic disorders while avoiding unwanted side effects …
GPR119 hold promise for treating metabolic disorders while avoiding unwanted side effects …
Dynamic insights into the self-activation pathway and allosteric regulation of the orphan G-protein-coupled receptor GPR52
Within over 800 members of G-protein-coupled receptors, there are numerous orphan
receptors whose endogenous ligands are largely unknown, providing many opportunities for …
receptors whose endogenous ligands are largely unknown, providing many opportunities for …
A native PAGE assay for the biochemical characterization of G protein coupling to GPCRs
AM Roehrkasse, JA Karim, AA Pioszak - Bio-protocol, 2021 - bio-protocol.org
G protein-coupled receptors (GPCRs) are a large family of membrane-embedded receptors
that have diverse roles in physiology and are major drug targets. GPCRs transduce an …
that have diverse roles in physiology and are major drug targets. GPCRs transduce an …
FLIM–FRET-Based Structural Characterization of a Class-A GPCR Dimer in the Cell Membrane
J Yang, Z Gong, YB Lu, CJ Xu, TF Wei, MS Yang… - Journal of molecular …, 2020 - Elsevier
Class-A G protein-coupled receptors (GPCRs) are known to homo-dimerize in the
membrane. Yet, methods to characterize the structure of GPCR dimer in the native …
membrane. Yet, methods to characterize the structure of GPCR dimer in the native …
Structural basis for G protein-coupled receptor activation
G protein-coupled receptors (GPCRs) are critical regulators of human physiology and make
up the largest single class of therapeutic drug targets. Although GPCRs regulate highly …
up the largest single class of therapeutic drug targets. Although GPCRs regulate highly …
A closer look into G protein coupled receptor activation: X-ray crystallography and long-scale molecular dynamics simulations
S Vanni, U Rothlisberger - Current medicinal chemistry, 2012 - ingentaconnect.com
G protein coupled receptors (GPCRs) are a large eukaryotic protein family of
transmembrane receptors that react to a signal coming from the extracellular environment to …
transmembrane receptors that react to a signal coming from the extracellular environment to …
Mechanistic insights into GPCR–G protein interactions
JP Mahoney, RK Sunahara - Current opinion in structural biology, 2016 - Elsevier
Highlights•Both GPCRs and G proteins sample multiple conformations in their basal
states.•Stabilizing a fully active state of several GPCRs requires agonist and G …
states.•Stabilizing a fully active state of several GPCRs requires agonist and G …
Bidirectional, iterative approach to the structural delineation of the functional “chemoprint” in GPR40 for agonist recognition
IG Tikhonova, CS Sum, S Neumann… - Journal of medicinal …, 2007 - ACS Publications
GPR40, free fatty acid receptor 1 (FFAR1), is a member of the GPCR superfamily and a
possible target for the treatment of type 2 diabetes. In this work, we conducted a bidirectional …
possible target for the treatment of type 2 diabetes. In this work, we conducted a bidirectional …
Unraveling the Functional Significance of Unstructured Regions in G Protein-Coupled Receptors
R Maggio, I Fasciani, F Petragnano, MF Coppolino… - Biomolecules, 2023 - mdpi.com
Unstructured regions in functional proteins have gained attention in recent years due to
advancements in informatics tools and biophysical methods. G protein-coupled receptors …
advancements in informatics tools and biophysical methods. G protein-coupled receptors …