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G protein-coupled receptors: a century of research and discovery
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 …
are the largest receptor family in the human genome, with≈ 800 members. GPCRs regulate …
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 …
The reactome pathway knowledgebase 2022
Abstract The Reactome Knowledgebase (https://reactome. org), an Elixir core resource,
provides manually curated molecular details across a broad range of physiological and …
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 …
normal and pathological brain function. In this regard, chemogenetic technologies represent …
How ligands illuminate GPCR molecular pharmacology
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 …
synthetic ligands, represent the largest family of druggable targets in the human genome …
Autoregulation of GPCR signalling through the third intracellular loop
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 …
for the signal transduction process downstream of receptor activation,–. Despite this, the lack …
Ligand and G-protein selectivity in the κ-opioid receptor
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 …
only pain but also addiction and affective disorders. However, the development of KOR …
Structural insights into µ-opioid receptor activation
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 …
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
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 …
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 …
desensitization and intracellular trafficking of G protein–coupled receptors (GPCRs), have …