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Crystal Structure of the β2Adrenergic Receptor-Gs protein complex
TLDR
This crystal structure represents the first high-resolution view of transmembrane signalling by a GPCR and the most surprising observation is a major displacement of the α-helical domain of Gαs relative to the Ras-like GTPase domain.
High-resolution crystal structure of an engineered human beta2-adrenergic G protein-coupled receptor.
TLDR
Although the location of carazolol in the beta2-adrenergic receptor is very similar to that of retinal in rhodopsin, structural differences in the ligand-binding site and other regions highlight the challenges in using rhodopin as a template model for this large receptor family.
Three-dimensional structure of the neuronal-Sec1–syntaxin 1a complex
TLDR
The crystal structure of the nSec1–syntaxin 1a complex, determined at 2.6 Å resolution, reveals that major conformational rearrangements occur in syntaxin relative to both the core SNARE complex and isolated syntaxin.
High-Resolution Crystal Structure of an Engineered Human β2-Adrenergic G Protein–Coupled Receptor
TLDR
Although the location of carazolol in the β2-adrenergic receptor is very similar to that of retinal in rhodopsin, structural differences in the ligand-binding site and other regions highlight the challenges in using rhodopin as a template model for this large receptor family.
Structure of a nanobody-stabilized active state of the β2 adrenoceptor
TLDR
A camelid antibody fragment to the human β2 adrenergic receptor is generated, and an agonist-bound, active-state crystal structure of the receptor-nanobody complex is obtained, providing insights into the process of agonist binding and activation.
Crystal structure of the μ-opioid receptor bound to a morphinan antagonist
TLDR
The 2.8 Å crystal structure of the mouse µ-OR in complex with an irreversible morphinan antagonist is described, revealing high-resolution insights into opioid receptor structure that will enable the application of structure-based approaches to develop better drugs for the management of pain and addiction.
Munc18a controls SNARE assembly through its interaction with the syntaxin N‐peptide
TLDR
It is shown that the syntaxin 16 N‐peptide binds to the SM protein Vps45, but the remainder of syntax in 16 strongly enhances the affinity of the interaction, which suggests that Munc18a controls the accessibility of syntaxin 1a to its partners.
GPCR Engineering Yields High-Resolution Structural Insights into β2-Adrenergic Receptor Function
TLDR
Analysis of adrenergic receptor ligand-binding mutants within the context of the reported high-resolution structure of β2AR-T4L provides insights into inverse-agonist binding and the structural changes required to accommodate catecholamine agonists.
Crystal structure of the human beta2 adrenergic G-protein-coupled receptor.
TLDR
The human beta2 adrenoceptor (beta2AR), which was crystallized in a lipid environment when bound to an inverse agonist and in complex with a Fab that binds to the third intracellular loop, differs from rhodopsin in having weaker interactions between the cytoplasmic ends of transmembrane (TM)3 and TM6, involving the conserved E/DRY sequences.
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