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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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Published in:Trends in pharmacological sciences (Regular ed.) 2020-06, Vol.41 (6), p.387-389
Main Authors: Yoo, Sungsoo M., Bhardwaj, Anshul, Benovic, Jeffrey L.
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description 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.
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subjects 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
title Arresting Developments in Biased Signaling
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