Mediaspace scheduled maintenance: Aug 25, 2026 07:00 - 12:00 AM. During this time, videos will be temporarily unavailable. Check status updates.

Concept

Allosteric modulator

Publications associées (26)

The Molecular Mechanism of P2Y 1 Receptor Activation

Horst Arthur Vogel, Shuguang Yuan

Human purinergic Gprotein-coupled receptor P2Y(1) (P2Y(1)R) is activated by adenosine 5'-diphosphate (ADP) to induce platelet activation and thereby serves as an important antithrombotic drug target. Crystal structures of P2Y(1)R revealed that one ligand ( ...

Wiley-Blackwell2016

Identification of genetic determinants and pharmacological modulators of mitochondrial function

Pénélope Andreux

Increased life expectancy goes hand in hand with a higher incidence of age-related diseases that affect the nervous and metabolic systems, such as type 2 diabetes, cancer, Parkinson’s and Alzheimer’s disease. These complex diseases are a product of the com ...

EPFL2013

Large scale expression and purification of the mouse 5-HT3 receptor

Horst Arthur Vogel, Cédric Deluz, Ghérici Hassaïne, Menno Berend Tol

Receptors of the Cys-loop family are central to neurotransmission and primary therapeutic targets. In order to decipher their gating and modulation mechanisms, structural data is essential. However, structural studies require large amounts of pure, functio ...

Elsevier Science Bv2013

Increasing the Efficiency of Ligands for FK506-Binding Protein 51 by Conformational Control

Ranganath Gopalakrishnan

The design of efficient ligands remains a key challenge in drug discovery. In the quest for lead-like ligands for the FK506-binding protein 51 (FKBP51), we designed two new classes of bicyclic sulfonamides to probe the contribution of conformational energy ...

Amer Chemical Soc2013

A Fluorescent Sensor for GABA and Synthetic GABA(B) Receptor Ligands

Kai Johnsson, Luc Reymond, Anastasiya Masharina

While gamma-aminobutyric acid (GABA) is the main inhibitory neurotransmitter, suitable tools to measure its concentration in living cells with high spatiotemporal resolution are missing. Herein, we describe the first ratiometric fluorescent sensor for GABA ...

American Chemical Society2012

SNAP-tag based FRET Indicator for GABA and Synthetic GABAB Receptor Ligands

Anastasiya Masharina

Whilst γ-aminobutyric acid (GABA) is the main inhibitory neurotransmitter in the central nervous system (CNS), suitable tools to measure its concentration in living cells with high spatiotemporal resolution are missing. This thesis describes the first rati ...

EPFL2012