Publications related to Inverse agonist

W246(6.48) Opens a Gate for a Continuous Intrinsic Water Pathway during Activation of the Adenosine A(2A) Receptor

The question how G-protein-coupled receptors transduce an extracellular signal by a sequence of transmembrane conformational transitions into an intracellular response remains to be solved at molecular detail. Herein, we use molecular dynamics simulations ...

Wiley-V C H Verlag Gmbh2015

Elucidating the Role of Site-Specific Nitration of alpha-Synuclein in the Pathogenesis of Parkinson's Disease via Protein Semisynthesis and Mutagenesis

Hilal Lashuel, Nadine Aït Bouziad, Anass Chiki, Ritwik Burai

Parkinsons disease (PD) is characterized by the loss of dopaminergic neurons in the substantia nigra and the presence of intraneuronal inclusions consisting of aggregated and post-translationally modified a-synuclein (a-syn). Despite advances in the chemic ...

Amer Chemical Soc2015

Peptide ligands stabilized by small molecules

Christian Heinis, Florence Pojer, Alessandro Angelini, Shiyu Chen, Davide Bertoldo

Bicyclic peptides generated through directed evolution by using phage display offer an attractive ligand format for the development of therapeutics. Being nearly 100-fold smaller than antibodies, they promise advantages such as access to chemical synthesis ...

Wiley-V C H Verlag Gmbh2014

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

Kai Johnsson, Luc Reymond, Keitaro Umezawa, 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

Cell-type-specific 2 adrenergic receptor clusters identified using photo-activated localization microscopy are not lipid raft related, but depend on actin cytoskeleton integrity

Aleksandra Radenovic, Paolo Annibale, Marco Scarselli

Recent developments in the field of optical super-resolution techniques allow both a 10-fold increase in resolution as well as an increased ability to quantify the number of labeled molecules visualized in the fluorescence measurement. By using photoactiva ...

2012

Predicting Novel Binding Modes of Agonists to β Adrenergic Receptors Using All-Atom Molecular Dynamics Simulations

Ursula Röthlisberger, Ivano Tavernelli, Marilisa Neri, Stefano Vanni

Understanding the binding mode of agonists to adrenergic receptors is crucial to enabling improved rational design of new therapeutic agents. However, so far the high conformational flexibility of G protein-coupled receptors has been an obstacle to obtaini ...

Public Library of Science2011

Ligand binding transmits conformational changes across the membrane-spanning region to the intracellular side of the 5-HT3 serotonin receptor

Horst Vogel, Horst Pick, Cédric Deluz, Erwin Ilegems

Conformational changes of channel activation: Five enhanced green fluorescent protein (EGFP) mols. (green cylinders) were integrated into the intracellular part of the homopentameric ionotropic 5-HT3 receptor. This allowed the detection of extracellular bi ...

2005

Oligomerization of the alpha 1a- and alpha 1b-Adrenergic Receptor Subtypes: Potential Implications in Receptor Internalization

Horst Vogel, Susanna Cotecchia, Laura Stanasila, Jean-Baptiste Perez

We combined biophys., biochem., and pharmacol. approaches to investigate the ability of the a1a- and a1b-adrenergic receptor (AR) subtypes to form homo- and hetero-oligomers. Receptors tagged with different epitopes (hemagglutinin and Myc) or fluorescent p ...

2003

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Inverse agonist

W246(6.48) Opens a Gate for a Continuous Intrinsic Water Pathway during Activation of the Adenosine A(2A) Receptor

Elucidating the Role of Site-Specific Nitration of alpha-Synuclein in the Pathogenesis of Parkinson's Disease via Protein Semisynthesis and Mutagenesis

Peptide ligands stabilized by small molecules

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

Cell-type-specific 2 adrenergic receptor clusters identified using photo-activated localization microscopy are not lipid raft related, but depend on actin cytoskeleton integrity

Predicting Novel Binding Modes of Agonists to β Adrenergic Receptors Using All-Atom Molecular Dynamics Simulations

Structure and function of the nicotinic acetylcholine receptor

Functional characterization of a human odorant receptor

Ligand binding transmits conformational changes across the membrane-spanning region to the intracellular side of the 5-HT3 serotonin receptor

Oligomerization of the alpha 1a- and alpha 1b-Adrenergic Receptor Subtypes: Potential Implications in Receptor Internalization

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Functional characterization of a human odorant receptor

Peptide ligands stabilized by small molecules

Cell-type-specific 2 adrenergic receptor clusters identified using photo-activated localization microscopy are not lipid raft related, but depend on actin cytoskeleton integrity

Structure and function of the nicotinic acetylcholine receptor

Ligand binding transmits conformational changes across the membrane-spanning region to the intracellular side of the 5-HT3 serotonin receptor

Oligomerization of the alpha 1a- and alpha 1b-Adrenergic Receptor Subtypes: Potential Implications in Receptor Internalization

Predicting Novel Binding Modes of Agonists to β Adrenergic Receptors Using All-Atom Molecular Dynamics Simulations

W246(6.48) Opens a Gate for a Continuous Intrinsic Water Pathway during Activation of the Adenosine A(2A) Receptor

Elucidating the Role of Site-Specific Nitration of alpha-Synuclein in the Pathogenesis of Parkinson's Disease via Protein Semisynthesis and Mutagenesis

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