G protein-coupled receptors: a century of research and discovery

S Liu, PJ Anderson, S Rajagopal, RJ Lefkowitz… - Circulation …, 2024 - ahajournals.org
GPCRs (G protein-coupled receptors), also known as 7 transmembrane domain receptors,
are the largest receptor family in the human genome, with≈ 800 members. GPCRs regulate …

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 reactome pathway knowledgebase 2022

M Gillespie, B Jassal, R Stephan, M Milacic… - Nucleic acids …, 2022 - academic.oup.com
Abstract The Reactome Knowledgebase (https://reactome. org), an Elixir core resource,
provides manually curated molecular details across a broad range of physiological and …

DREADDs for neuroscientists

BL Roth - Neuron, 2016 - cell.com
To understand brain function, it is essential that we discover how cellular signaling specifies
normal and pathological brain function. In this regard, chemogenetic technologies represent …

How ligands illuminate GPCR molecular pharmacology

D Wacker, RC Stevens, BL Roth - Cell, 2017 - cell.com
G protein-coupled receptors (GPCRs), which are modulated by a variety of endogenous and
synthetic ligands, represent the largest family of druggable targets in the human genome …

Autoregulation of GPCR signalling through the third intracellular loop

F Sadler, N Ma, M Ritt, Y Sharma, N Vaidehi… - Nature, 2023 - nature.com
The third intracellular loop (ICL3) of the G protein-coupled receptor (GPCR) fold is important
for the signal transduction process downstream of receptor activation,–. Despite this, the lack …

Ligand and G-protein selectivity in the κ-opioid receptor

J Han, J Zhang, AL Nazarova, SM Bernhard… - Nature, 2023 - nature.com
The κ-opioid receptor (KOR) represents a highly desirable therapeutic target for treating not
only pain but also addiction and affective disorders. However, the development of KOR …

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 …

[HTML][HTML] Mini G protein probes for active G protein–coupled receptors (GPCRs) in live cells

Q Wan, N Okashah, A Inoue, R Nehmé… - Journal of Biological …, 2018 - Elsevier
G protein–coupled receptors (GPCRs) are key signaling proteins that regulate nearly every
aspect of cell function. Studies of GPCRs have benefited greatly from the development of …

The diverse roles of arrestin scaffolds in G protein–coupled receptor signaling

YK Peterson, LM Luttrell - Pharmacological reviews, 2017 - Elsevier
The visual/β-arrestins, a small family of proteins originally described for their role in the
desensitization and intracellular trafficking of G protein–coupled receptors (GPCRs), have …