G protein–coupled receptor kinases (GRKs) orchestrate biased agonism at the β2-adrenergic receptor

Sortase ligation enables homogeneous GPCR phosphorylation to reveal diversity in β-arrestin coupling

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Trends in GPCR drug discovery: new agents, targets and indications

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Distinct conformations of GPCR–β-arrestin complexes mediate desensitization, signaling, and endocytosis

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Allosteric coupling from G protein to the agonist-binding pocket in GPCRs

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GPCRdb: an information system for G protein-coupled receptors

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Functional competence of a partially engaged GPCR–β-arrestin complex

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Structural insights into µ-opioid receptor activation

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

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Pioneering biased ligand offers efficacy with reduced on-target toxicity

(2015) Katie Kingwell   NATURE REVIEWS DRUG DISCOVERY

Elucidation of G-protein and β-arrestin functional selectivity at the dopamine D2 receptor

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Biased agonism of the μ-opioid receptor by TRV130 increases analgesia and reduces on-target adverse effects versus morphine: A randomized, double-blind, placebo-controlled, crossover study in healthy volunteers

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Structure of active β-arrestin-1 bound to a G-protein-coupled receptor phosphopeptide

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Quantifying Ligand Bias at Seven-Transmembrane Receptors

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Structure of a nanobody-stabilized active state of the β2 adrenoceptor

(2011) Søren G. F. Rasmussen et al.   NATURE

Crystal structure of the β2 adrenergic receptor–Gs protein complex

(2011) Søren G. F. Rasmussen et al.   NATURE

Distinct Phosphorylation Sites on the  2-Adrenergic Receptor Establish a Barcode That Encodes Differential Functions of  -Arrestin

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Emerging paradigms of β-arrestin-dependent seven transmembrane receptor signaling

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Structural insights into adrenergic receptor function and pharmacology

(2011) Brian K. Kobilka   TRENDS IN PHARMACOLOGICAL SCIENCES

New perspectives regarding β2-adrenoceptor ligands in the treatment of asthma

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Teaching old receptors new tricks: biasing seven-transmembrane receptors

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Therapeutic potential of β-arrestin- and G protein-biased agonists

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