Abstract
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.
Keywords:
G protein-coupled receptor; arrestin; cryo-EM.
Copyright © 2020 Elsevier Ltd. All rights reserved.
Publication types
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Research Support, N.I.H., Extramural
MeSH terms
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Animals
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Biomimetic Materials / chemistry
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Humans
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Models, Molecular
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Molecular Targeted Therapy
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Receptors, Adrenergic, beta-1 / chemistry
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Receptors, Adrenergic, beta-1 / metabolism
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Receptors, G-Protein-Coupled / agonists*
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Receptors, G-Protein-Coupled / chemistry*
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Receptors, G-Protein-Coupled / metabolism
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Signal Transduction / drug effects
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Single-Domain Antibodies / chemistry
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beta-Arrestin 1 / chemistry*
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beta-Arrestin 1 / metabolism
Substances
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Receptors, Adrenergic, beta-1
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Receptors, G-Protein-Coupled
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Single-Domain Antibodies
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beta-Arrestin 1