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Gαi1 inhibition mechanism of ATP-bound adenylyl cyclase type 5

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Exploring the inhibition mechanism of adenylyl cyclase type 5 by n-terminal myristoylated Gαi1

Ursula Röthlisberger, Siri Camee van Keulen

Adenylyl cyclase (AC) is an important messenger involved in G-protein-coupled-receptor signal transduction pathways, which is a well-known target for drug development. AC is regulated by activated stimulatory (Gαs) and inhibitory (Gαi) G proteins in the cy ...

Public Library of Science2017

Effect of N-Terminal Myristoylation on the Active Conformation of Gα

Ursula Röthlisberger, Siri Camee van Keulen

G proteins are part of the G-protein-coupled receptor (GPCR) signal transduction cascade in which they transfer a signal from the membrane-embedded GPCR to other proteins in the cell. In the case of the inhibitory G-protein heterotrimer, permanent N-termin ...

2017

AMP-activated protein kinase

Serge Thanh Son Ducommun

AMP-activated protein kinase (AMPK) is an evolutionally conserved key sensor of cellular energy status. Under conditions of cellular energy stress, AMPK is activated and will switch off anabolic processes that consume ATP, while activating catabolic proces ...

EPFL2016

Identification of genetic interactors of ypa2 in Schizosaccharomyces pombe

Manuela Moraru

In this study, the fission yeast Schizosaccharomyces pombe was used as a model system to study the cellular signaling that underlies cell cycle progression. Phosphorylation plays an important part in the regulation of this process. Kinases catalyze the tra ...

EPFL2016

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

Horst Vogel, Shuguang Yuan, Zhenquan Hu

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

Background: Ras nanoclusters contain 6-8 Ras proteins on the plasma membrane and serve as indispensable signaling platforms for Ras-MAPK signaling. Results: Ras membrane conformer mutants impart specific galectin-1-dependent nanoclustering responses. Concl ...

American Society for Biochemistry and Molecular Biology2014

Background: The mechanism of ligand gating in physiologically important cyclic nucleotide-modulated channels is unknown. Results: We constructed and purified a chimeric ion channel with activity modulated by cAMP and used it to measure ligand-binding energ ...

American Society for Biochemistry & Molecular Biology (ASBMB)2014

Assembly of the Transmembrane Domain of E. coli PhoQ Histidine Kinase: Implications for Signal Transduction from Molecular Simulations

Matteo Dal Peraro, Thomas Lemmin

The PhoQP two-component system is a signaling complex essential for bacterial virulence and cationic antimicrobial peptide resistance. PhoQ is the histidine kinase chemoreceptor of this tandem machine and assembles in a homodimer conformation spanning the ...

Public Library Science2013

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

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