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 …

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 …

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 …

Structure of the µ-opioid receptor–Gi protein complex

A Koehl, H Hu, S Maeda, Y Zhang, Q Qu, JM Paggi… - Nature, 2018 - nature.com
The μ-opioid receptor (μOR) is a G-protein-coupled receptor (GPCR) and the target of most
clinically and recreationally used opioids. The induced positive effects of analgesia and …

Structural insights into µ-opioid receptor activation

W Huang, A Manglik, AJ Venkatakrishnan… - Nature, 2015 - nature.com
Activation of the μ-opioid receptor (μOR) is responsible for the efficacy of the most effective
analgesics. To shed light on the structural basis for μOR activation, here we report a 2.1 Å X …

Crystal structure of rhodopsin bound to arrestin by femtosecond X-ray laser

Y Kang, XE Zhou, X Gao, Y He, W Liu, A Ishchenko… - Nature, 2015 - nature.com
G-protein-coupled receptors (GPCRs) signal primarily through G proteins or arrestins.
Arrestin binding to GPCRs blocks G protein interaction and redirects signalling to numerous …

Structures of the M1 and M2 muscarinic acetylcholine receptor/G-protein complexes

S Maeda, Q Qu, MJ Robertson, G Skiniotis, BK Kobilka - Science, 2019 - science.org
Muscarinic acetylcholine receptors are G protein–coupled receptors that respond to
acetylcholine and play important signaling roles in the nervous system. There are five …

Structure of the adenosine-bound human adenosine A1 receptor–Gi complex

CJ Draper-Joyce, M Khoshouei, DM Thal, YL Liang… - Nature, 2018 - nature.com
The class A adenosine A1 receptor (A1R) is a G-protein-coupled receptor that preferentially
couples to inhibitory Gi/o heterotrimeric G proteins, has been implicated in numerous …

[HTML][HTML] Structural insights into the dynamic process of β2-adrenergic receptor signaling

A Manglik, TH Kim, M Masureel, C Altenbach, Z Yang… - Cell, 2015 - cell.com
G-protein-coupled receptors (GPCRs) transduce signals from the extracellular environment
to intracellular proteins. To gain structural insight into the regulation of receptor cytoplasmic …

Structural insights into G-protein-coupled receptor allostery

DM Thal, A Glukhova, PM Sexton, A Christopoulos - Nature, 2018 - nature.com
G-protein-coupled receptors (GPCRs) are key cell-surface proteins that transduce external
environmental cues into biochemical signals across the membrane. GPCRs are intrinsically …