Publication

The Principles of Ligand Specificity on beta-2-adrenergic receptor

Publications associées (118)

Exploring G-Protein Coupled Receptor Activation with Multiscale Molecular Simulations

This thesis is devoted to the study of the activation mechanism of G-protein coupled receptors (GPCRs), one of the largest and most diverse protein families in mammalian genomes, by means of different computer-based simulation techniques. Using force field ...

EPFL2011

Advanced Fluorescence Microscopy to Study Plasma Membrane Protein Dynamics

Joachim Piguet

Membrane protein dynamics is of great importance for living organisms. The precise localization of proteins composing a synapse on the membrane facing a nerve terminus is essential for proper functioning of the nervous system. In muscle fibers, the nicotin ...

EPFL2010

Bioanalytical procedure to detect membrane receptor activation

Horst Vogel, Horst Pick

The invention concerns a method for screening compound interaction with transmembrane receptors involved in cellular signal transduction, preferably with G protein coupled receptors, by adding the compound to be analyzed into a medium comprising native inv ...

2010

A conserved protonation-induced switch can trigger "ionic lock" formation in adrenergic receptors

Ursula Röthlisberger, Ivano Tavernelli, Marilisa Neri, Stefano Vanni

The mechanism of signal transduction in G-protein-coupled receptors (GPCRs) is a crucial step in cell signaling. However, the molecular details of this process are still largely undetermined. Carrying out submicrosecond molecular dynamics simulations of be ...

Elsevier2010

Improving Protein Pharmacokinetics by Engineering Erythrocyte Affinity

Stephane Kontos, Jeffrey Alan Hubbell

Poor pharmacokinetic profiles are often the underlying reason for the failure of novel protein drugs to reach clinical translation. Current passive half-life improvement methods focus on increasing the apparent hydrodynamic radius of the drug. We sought to ...

American Chemical Society2010

Role of Aggregation in Rhodopsin Signal Transduction

Ursula Röthlisberger, Ivano Tavernelli, Marilisa Neri, Stefano Vanni

Many G protein-coupled receptors (GPCRs) are known to form dimers or even oligomers, and these aggregated states have been proposed as functional units responsible for signal transduction and G protein activation. However, the nature of their involvement h ...

2010

Rational Design of Indoleamine 2,3-Dioxygenase Inhibitors

Pierre Vogel, Loay Awad, Olivier Michielin

Indoleamine 2,3-dioxygenase (IDO) is an important therapeutic target for the treatment of diseases such as cancer that involve pathological immune escape. We have used the evolutionary docking algorithm EADock to design new inhibitors of this enzyme. First ...

2010

Hybrid Polymer Therapeutics Incorporating Bioresponsive, Coiled Coil Peptide Linkers

Harm-Anton Klok

This article reports the design, synthesis and results of first in vitro model studies of a conceptually novel class of polymer therapeutics in which the cargo is attached to a polymer backbone via a noncovalent, biologically inspired coiled coil linker, w ...

American Chemical Society2010

Rhodium(I)-Catalyzed 1,4-Silicon Shift of Unactivated Silanes from Aryl to Alkyl: Enantioselective Synthesis of Indanol Derivatives

Nicolai Cramer

Enantioselective Rh-promoted activation and 1,4-positional swap of unactivated tetraorganosilanes, e.g., 1-ethyl-3-methyl-3-(2-(trimethylsilyl)phenyl)cyclobutanol (I) to give (1S,3S)-1-ethyl-3-methyl-3((trimethylsilyl)methyl)indanol (II). E.g., reaction of ...

Wiley-VCH Verlag GmbH & Co. KGaA2010

GRASP65 and GRASP55 Sequentially Promote the Transport of C-terminal Valine-bearing Cargos to and through the Golgi Complex

Giovanni D'Angelo

The Golgi matrix proteins GRASP65 and GRASP55 have recognized roles in maintaining the architecture of the Golgi complex, in mitotic progression and in unconventional protein secretion whereas, surprisingly, they have been shown to be dispensable for the t ...

2009

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