Publication

The Mechanism of Ligand-Induced Activation or Inhibition of - and -Opioid Receptors

Publications associées (28)

Reprogramming G Protein-Coupled Receptor Structure, Function And Signaling By Computational Design

G protein-coupled receptors (GPCRs) are 7-transmembrane alpha-helical integral membrane proteins on which cells heavily rely to receive information regarding their external environment. These receptors are able to transfer information to intracellular down ...

EPFL2021

Structural basis of the activation of the CC chemokine receptor 5 by a chemokine agonist

Henning Paul-Julius Stahlberg, Nicolas Calo, Polina Isaikina

The human CC chemokine receptor 5 (CCR5) is a G protein-coupled receptor (GPCR) that plays a major role in inflammation and is involved in cancer, HIV, and COVID-19. Despite its importance as a drug target, the molecular activation mechanism of CCR5, i.e., ...

AMER ASSOC ADVANCEMENT SCIENCE2021

The role of metal ions in G protein-coupled receptor signalling and drug discovery

Horst Vogel, Shuguang Yuan, Xueying Wang

Metal ions, such as Na+, Mg2+, Ca2+, and Zn2+, are highly abundant in biological systems. For many G protein-coupled receptors (GPCRs), metal ions, especially Na+, have been found to stabilize the receptors' inactivate state preventing receptor activation. ...

WILEY2021

Allosteric modulators enhance agonist efficacy by increasing the residence time of a GPCR in the active state

Anne-Marinette Thi Phuong Hanh Cao

Here, the authors use smFRET to assess the structural dynamics of metabotropic glutamate receptor mGlu2 and show that a positive allosteric modulator or the Gi protein stabilize mGlu2 in the glutamate-induced active state, leading to the full activation of ...

Nature Portfolio2021

Asymmetric opening of the homopentameric 5-HT3A serotonin receptor in lipid bilayers

Horst Vogel, Shuguang Yuan

Pentameric ligand-gated ion channels (pLGICs) of the Cys-loop receptor family are key players in fast signal transduction throughout the nervous system. They have been shown to be modulated by the lipid environment, however the underlying mechanism is not ...

Nature Research2021

The Mammalian Membrane Microenvironment Regulates the Sequential Attachment of Bacteria to Host Cells

Alexandre Louis André Persat, Xavier Jean-Yves Pierrat, Jeremy Pak Hei Wong

Pathogen attachment to host tissue is critical in the progress of many infections. Bacteria use adhesion in vivo to stabilize colonization and subsequently regulate the deployment of contact-dependent virulence traits. To specifically target host cells, th ...

2021

Golgi maturation-dependent glycoenzyme recycling controls glycosphingolipid biosynthesis and cell growth via GOLPH3

Anthony Vocat, Giovanni D'Angelo, Laura Capolupo, Riccardo Rizzo

Glycosphingolipids are important components of the plasma membrane where they modulate the activities of membrane proteins including signalling receptors. Glycosphingolipid synthesis relies on competing reactions catalysed by Golgi-resident enzymes during ...

WILEY2021

Ligand Effects in Low-Valent Co(I) Clathrochelate Complexes

Kay Severin, Rosario Scopelliti, Farzaneh Fadaei Tirani, Ophélie Marie Planes

Clathrochelate complexes of cobalt are known in the oxidation states I, II, and III. Low-valent Co(I) complexes are highly reactive compounds, and there is only limited knowledge about their structures in the solid state. Herein, we describe the crystallog ...

2021