Results 111 to 120 of about 851,179 (309)

Dynamic tuneable G protein-coupled receptor monomer-dimer populations

Nature Communications, 2018
Evidence suggests oligomerisation of G protein-coupled receptors in membranes, but this is controversial. Here, authors use single-molecule and ensemble FRET, and spectroscopy to show that the neurotensin receptor 1 forms multiple dimer conformations ...
Patricia M. Dijkman, Oliver K. Castell, Alan D. Goddard, Juan C. Munoz-Garcia, Chris de Graaf, Mark I. Wallace, Anthony Watts   +6 more
doaj   +1 more source

Alamandine and Its Receptor MrgD Pair Up to Join the Protective Arm of the Renin-Angiotensin System [PDF]

, 2019
Only a few years ago, alamandine was found to be a member of the protective arm of the renin-angiotensin system. It turned out to be an endogenous ligand of the G protein-coupled receptor MrgD.
Schleifenbaum, Johanna
core   +1 more source

An unexpected alternative viologen electron mediator site in tungsten‐containing formate dehydrogenase

FEBS Letters, EarlyView.
An unexpected alternative interaction site for ethyl viologen was identified in formate dehydrogenase 1 from Methylorubrum extorquens. Combined mutagenesis, kinetic analysis, and docking revealed that aromatic residues near an iron–sulfur cluster enable flavin mononucleotide‐independent electron transfer, offering a framework for engineering improved ...
Eleni G. Poloniataki, Yong Hwan Kim
wiley   +1 more source

Measuring ligand efficacy at the mu-opioid receptor using a conformational biosensor. [PDF]

, 2018
The intrinsic efficacy of orthosteric ligands acting at G-protein-coupled receptors (GPCRs) reflects their ability to stabilize active receptor states (R*) and is a major determinant of their physiological effects.
Livingston, Kathryn E, Mahoney, Jacob P, Manglik, Aashish, Sunahara, Roger K, Traynor, John R   +4 more
core  

G protein-coupled receptor 35: an emerging target in inflammatory and cardiovascular disease [PDF]

, 2015
G protein-coupled receptor 35 (GPR35) is an orphan receptor, discovered in 1998, that has garnered interest as a potential therapeutic target through its association with a range of diseases.
Amanda E Mackenzie, Graeme eMilligan, Nina eDivorty, Nina eDivorty, Stuart A. Nicklin   +4 more
core   +3 more sources

Ubiquitination of secretory granules promotes their crinophagic degradation in Drosophila

FEBS Letters, EarlyView.
Ubiquitination of secretory granules in Drosophila larval salivary glands is a critical molecular trigger for crinophagy, the lysosomal degradation of unreleased, or low‐quality granules. The E3 ubiquitin ligase Cnot4 is recruited to the surface of secretory granules to induce crinophagy.
Tamás Csizmadia, Anna Dósa, Asha Kiran Maddali, András Jipa, Hajnalka Laczkó‐Dobos, Péter Lőw, Gábor Juhász   +6 more
wiley   +1 more source

Targeted elimination of G proteins and arrestins defines their specific contributions to both intensity and duration of G protein-coupled receptor signalling [PDF]

, 2016
G protein-coupled receptors (GPCRs) can initiate intracellular signalling cascades by coupling to an array of heterotrimeric G proteins and arrestin adaptor proteins. Understanding the contribution of each of these coupling options to GPCR signalling has
Alvarez-Curto, Elisa, Inoue, Asuka, Jenkins, Laura, Milligan, Graeme, Prihandoko, Rudi, Raihan, Sheikh Zahir, Tobin, Andrew B.   +6 more
core   +1 more source

Transcriptional network analysis of PTEN‐protein‐deficient prostate tumors reveals robust stromal reprogramming and signs of senescent paracrine communication

Molecular Oncology, Volume 20, Issue 6, Page 1429-1452, June 2026.
Combining PTEN protein assessment and transcriptomic profiling of prostate tumors, we uncovered a network enriched in senescence and extracellular matrix (ECM) programs associated with PTEN loss and conserved in a mouse model. We show that PTEN‐deficient cells trigger paracrine remodeling of the surrounding stroma and this information could help ...
Ivana Rondon‐Lorefice, Jose I. Lopez, Aitziber Ugalde‐Olano, Maite Zufiaurre, Ianire Astobiza, Natalia Martin‐Martin, Laura Bozal‐Basterra, Saioa Garcia‐Longarte, Amaia Zabala‐Letona, Sofia Rey, Aida Santos‐Martin, Miguel Unda, Ana Loizaga‐Iriarte, Mariona Graupera, Paolo Nuciforo, Arkaitz Carracedo, Isabel Mendizabal   +16 more
wiley   +1 more source

Biased antagonism of a series of bicyclic CXCR2 intracellular allosteric modulators

Frontiers in Pharmacology
Targeting the human chemokine receptor (CXCR2) holds significant potential in treating inflammatory diseases and cancer. In this study, we investigate the biased properties of previously reported CXCR2 antagonists (i.e., the MVH compounds).
Brent Van Bosstraeten, Katrijn Boon, Max Van Hoof, Wim Dehaen, Martyna Szpakowska, Andy Chevigné, Dominique Schols, Steven De Jonghe, Tom Van Loy   +8 more
doaj   +1 more source

Membrane cholesterol access into a G-protein-coupled receptor

Nature Communications, 2017
G-protein-coupled receptors trigger several signalling pathways and their activity was proposed to be allosteric modulated by cholesterol. Here the authors use molecular dynamics simulations and ligand binding assays to show that membrane cholesterol can
Ramon Guixà-González, José L. Albasanz, Ismael Rodriguez-Espigares, Manuel Pastor, Ferran Sanz, Maria Martí-Solano, Moutusi Manna, Hector Martinez-Seara, Peter W. Hildebrand, Mairena Martín, Jana Selent   +10 more
doaj   +1 more source