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Biased signalling: from simple switches to allosteric microprocessors
G protein-coupled receptors (GPCRs) are the largest class of receptors in the human
genome and some of the most common drug targets. It is now well established that GPCRs …
genome and some of the most common drug targets. It is now well established that GPCRs …
In-cell structural biology by NMR: the benefits of the atomic scale
FX Theillet - Chemical reviews, 2022 - ACS Publications
In-cell structural biology aims at extracting structural information about proteins or nucleic
acids in their native, cellular environment. This emerging field holds great promise and is …
acids in their native, cellular environment. This emerging field holds great promise and is …
Common activation mechanism of class A GPCRs
Class A G-protein-coupled receptors (GPCRs) influence virtually every aspect of human
physiology. Understanding receptor activation mechanism is critical for discovering novel …
physiology. Understanding receptor activation mechanism is critical for discovering novel …
GPCR dynamics: structures in motion
The function of G protein-coupled receptors (GPCRs) which represent the largest class of
both human membrane proteins and drug targets depends critically on their ability to …
both human membrane proteins and drug targets depends critically on their ability to …
The molecular basis of G protein–coupled receptor activation
G protein–coupled receptors (GPCRs) mediate the majority of cellular responses to external
stimuli. Upon activation by a ligand, the receptor binds to a partner heterotrimeric G protein …
stimuli. Upon activation by a ligand, the receptor binds to a partner heterotrimeric G protein …
Delineating the conformational landscape of the adenosine A2A receptor during G protein coupling
G-protein-coupled receptors (GPCRs) represent a ubiquitous membrane protein family and
are important drug targets. Their diverse signaling pathways are driven by complex …
are important drug targets. Their diverse signaling pathways are driven by complex …
GPCR drug discovery: integrating solution NMR data with crystal and cryo-EM structures
I Shimada, T Ueda, Y Kofuku, MT Eddy… - Nature Reviews Drug …, 2019 - nature.com
The 826 G protein-coupled receptors (GPCRs) in the human proteome regulate key
physiological processes and thus have long been attractive drug targets. With the crystal …
physiological processes and thus have long been attractive drug targets. With the crystal …
Nanobodies to study G protein–coupled receptor structure and function
Ligand-induced activation of G protein–coupled receptors (GPCRs) is a key mechanism
permitting communication between cells and organs. Enormous progress has recently …
permitting communication between cells and organs. Enormous progress has recently …
Allosteric coupling of drug binding and intracellular signaling in the A2A adenosine receptor
Signaling across cellular membranes, the 826 human G protein-coupled receptors (GPCRs)
govern a wide range of vital physiological processes, making GPCRs prominent drug …
govern a wide range of vital physiological processes, making GPCRs prominent drug …
The role of structural dynamics in GPCR‐mediated signaling
D Hilger - The FEBS journal, 2021 - Wiley Online Library
G protein‐coupled receptors (GPCRs) play critical roles in the regulation of human
physiology in response to a wide array of different extracellular stimuli and thus represent …
physiology in response to a wide array of different extracellular stimuli and thus represent …