Biased signalling: from simple switches to allosteric microprocessors

JS Smith, RJ Lefkowitz, S Rajagopal - Nature reviews Drug discovery, 2018 - nature.com
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 …

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 …

[HTML][HTML] Common activation mechanism of class A GPCRs

Q Zhou, D Yang, M Wu, Y Guo, W Guo, L Zhong, X Cai… - Elife, 2019 - elifesciences.org
Class A G-protein-coupled receptors (GPCRs) influence virtually every aspect of human
physiology. Understanding receptor activation mechanism is critical for discovering novel …

GPCR dynamics: structures in motion

NR Latorraca, AJ Venkatakrishnan, RO Dror - Chemical reviews, 2017 - ACS Publications
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 …

The molecular basis of G protein–coupled receptor activation

WI Weis, BK Kobilka - Annual review of biochemistry, 2018 - annualreviews.org
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 …

[HTML][HTML] Delineating the conformational landscape of the adenosine A2A receptor during G protein coupling

SK Huang, A Pandey, DP Tran, NL Villanueva, A Kitao… - Cell, 2021 - cell.com
G-protein-coupled receptors (GPCRs) represent a ubiquitous membrane protein family and
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 …

[HTML][HTML] Allosteric coupling of drug binding and intracellular signaling in the A2A adenosine receptor

MT Eddy, MY Lee, ZG Gao, KL White, T Didenko… - Cell, 2018 - cell.com
Signaling across cellular membranes, the 826 human G protein-coupled receptors (GPCRs)
govern a wide range of vital physiological processes, making GPCRs prominent drug …

Nanobodies to study G protein–coupled receptor structure and function

A Manglik, BK Kobilka, J Steyaert - Annual review of …, 2017 - annualreviews.org
Ligand-induced activation of G protein–coupled receptors (GPCRs) is a key mechanism
permitting communication between cells and organs. Enormous progress has recently …

[HTML][HTML] Hsp70 chaperone: a master player in protein homeostasis

MR Fernández-Fernández, JM Valpuesta - F1000Research, 2018 - ncbi.nlm.nih.gov
Protein homeostasis (proteostasis) is an essential pillar for correct cellular function.
Impairments in proteostasis are encountered both in aging and in several human disease …