Arresting Developments in Biased Signaling

The ability to design ‘biased’ drugs that selectively activate G protein-coupled receptor (GPCR) signaling pathways beneficial in treating a disease, while limiting their side effects, is of broad significance. Lee et al. move us a step closer to this important goal by identifying structural differe...

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Veröffentlicht in:	Trends in pharmacological sciences (Regular ed.) 2020-06, Vol.41 (6), p.387-389
Hauptverfasser:	Yoo, Sungsoo M., Bhardwaj, Anshul, Benovic, Jeffrey L.
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals arrestin beta-Arrestin 1 - chemistry beta-Arrestin 1 - metabolism Biomimetic Materials - chemistry cryo-EM G protein-coupled receptor Humans Models, Molecular Molecular Targeted Therapy Receptors, Adrenergic, beta-1 - chemistry Receptors, Adrenergic, beta-1 - metabolism Receptors, G-Protein-Coupled - agonists Receptors, G-Protein-Coupled - chemistry Receptors, G-Protein-Coupled - metabolism Signal Transduction - drug effects Single-Domain Antibodies - chemistry
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Beschreibung
Zusammenfassung:	The ability to design ‘biased’ drugs that selectively activate G protein-coupled receptor (GPCR) signaling pathways beneficial in treating a disease, while limiting their side effects, is of broad significance. Lee et al. move us a step closer to this important goal by identifying structural differences in the β1-adrenoceptor in complex with β-arrestin 1 versus a G protein-mimicking nanobody.
ISSN:	0165-6147 1873-3735
DOI:	10.1016/j.tips.2020.04.003