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Computationally designed GPCR quaternary structures bias signaling pathway activation

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Mechanistic Studies on the Stereoselectivity of the Serotonin 5-HT1A Receptor

Horst Vogel, Shuguang Yuan

G-protein-coupled receptors (GPCRs) are involved in a wide range of physiological processes, and they have attracted considerable attention as important targets for developing new medicines. A central and largely unresolved question in drug discovery, whic ...

Wiley-Blackwell2016

Revealing GPCR oligomerization at the single-molecule level through a nanoscopic lens: methods, dynamics and biological function

Aleksandra Radenovic, Paolo Annibale, Marco Scarselli

The introduction of super-resolution fluorescence microscopy has allowed the visualization of single proteins in their biological environment. Recently, these techniques have been applied to determine the organization of class A G-protein-coupled receptors ...

Wiley-Blackwell2015

Single-Molecule Imaging Deciphers the Relation between Mobility and Signaling of a Prototypical G Protein-Coupled Receptor in Living Cells

Horst Vogel, Joachim Piguet, Luc Veya

Lateral diffusion enables efficient interactions between membrane proteins leading to signal transmission across the plasma membrane. An open question is how the spatio-temporal distribution of cell surface receptors influences the transmembrane signaling ...

American Society for Biochemistry and Molecular Biology2015

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Precise regulation of the Notch signaling pathway is crucial, as increases or deficiencies in signaling are associated with diseases, including a wide range of cancers. Recent studies have demonstrated that monoclonal antibodies that bind and stabilize the ...

Wiley-Blackwell2015

Exchanging ligand-binding specificity between a pair of mouse olfactory receptor paralogs reveals odorant recognition principles

Horst Vogel, Horst Pick, Shuguang Yuan, Luc Veya, Olivia Baud

A multi-gene family of ~1000 G protein-coupled olfactory receptors (ORs) constitutes the molecular basis of mammalian olfaction. Due to the lack of structural data its remarkable capacity to detect and discriminate thousands of odorants remains poorly unde ...

Nature Publishing Group2015

Flagellated bacteria, such as Escherichia coli, perform directed motion in gradients of concentration of attractants and repellents in a process called chemotaxis. The E. coli chemotaxis signaling pathway is a model for signal transduction, but it has uniq ...

Elsevier BV2015

G protein-coupled receptors (GPCRs) are ubiquitous mediators of signal transduction across cell membranes and constitute a very important class of therapeutic targets. The main mechanisms involving GPCR activation and signal transduction to the cell interi ...

EPFL2013

Transmembrane Signaling Analysis in Model Membrane Systems

Luigino Grasso

Studying the complex mechanisms of transducing an extracellular signal across a plasma membrane to initiate an intracellular responce is of fundamental importance for a cell’s function. Transmembrane signaling is the key allowing cells to sense and communi ...

EPFL2012

A Biochemical and Biophysical Investigation of 5-HT3 Receptor Stability

Menno Berend Tol

The 5-hydroxytryptamine 3 receptor (5-HT3R) is a member of the pentameric ligand-gated ion channel (pLGIC) family, that plays an important role in fast signal transduction and cell-cell communication in synapses: They convert a chemical signal from a neuro ...

EPFL2012

A Closer Look into G Protein Coupled Receptor Activation: X-Ray Crystallography and Long-Scale Molecular Dynamics Simulations

Ursula Röthlisberger, Stefano Vanni

G protein coupled receptors (GPCRs) are a large eukaryotic protein family of transmembrane receptors that react to a signal coming from the extracellular environment to generate an intracellular response through the activation of a signal transduction path ...

2012