Results 11 to 20 of about 10,936,171 (356)

A saposin-lipoprotein nanoparticle system for membrane proteins. [PDF]

Nature Methods, 2016
A limiting factor in membrane protein research is the ability to solubilize and stabilize such proteins. Detergents are used most often for solubilizing membrane proteins, but they are associated with protein instability and poor compatibility with ...
Armache, Jean-Paul, Briggs, John AG, Cheng, Yifan, Flayhan, Ali, Frauenfeld, Jens, Garoff, Henrik, Guettou, Fatma, Jegerschöld, Caroline, Löving, Robin, Löw, Christian, Moberg, Per, Nordlund, Pär, Sonnen, Andreas F-P, Zhu, Lin   +13 more
core   +3 more sources

Regulation of membrane protein structure and function by their lipid nano-environment

Nature Reviews Molecular Cell Biology, 2022
I. Levental, E. Lyman
semanticscholar   +3 more sources

Combined docking and machine learning identify key molecular determinants of ligand pharmacological activity on β2 adrenoceptor

Pharmacology Research & Perspectives, 2022
G protein‐coupled receptors (GPCRs) are valuable therapeutic targets for many diseases. A central question of GPCR drug discovery is to understand what determines the agonism or antagonism of ligands that bind them.
Mireia Jiménez‐Rosés, Bradley Angus Morgan, Maria Jimenez Sigstad, Thuy Duong Zoe Tran, Rohini Srivastava, Asuman Bunsuz, Leire Borrega‐Román, Pattarin Hompluem, Sean A. Cullum, Clare R. Harwood, Eline J. Koers, David A. Sykes, Iain B. Styles, Dmitry B. Veprintsev   +13 more
doaj   +1 more source

Exploring the kinetic selectivity of drugs targeting the β1‐adrenoceptor

Pharmacology Research & Perspectives, 2022
In this study, we report the β1‐adrenoceptor binding kinetics of several clinically relevant β1/2‐adrenoceptor (β1/2AR) agonists and antagonists. [3H]‐DHA was used to label CHO‐β1AR for binding studies. The kinetics of ligand binding was assessed using a
David A. Sykes, Mireia Jiménez‐Rosés, John Reilly, Robin A. Fairhurst, Steven J. Charlton, Dmitry B. Veprintsev   +5 more
doaj   +1 more source

Reagents and models for detecting endogenous GLP1R and GIPR

EBioMedicine, 2021
Glucagon-like peptide-1 receptor (GLP1R) agonists target the GLP1R, whereas dual GLP1R/ gastric inhibitory polypeptide receptor (GIPR) agonists target both the GLP1R and GIPR. Despite the importance of these drug classes for the treatment of diabetes and
Julia Ast, Johannes Broichhagen, David J. Hodson   +2 more
doaj   +1 more source

Revealing the tissue-level complexity of endogenous glucagon-like peptide-1 receptor expression and signaling

Nature Communications, 2023
Visualizing endogenous GPCRs is challenging. Here the authors generate mice with an enzyme self-label genome-edited into the endogenous glucagon-like peptide-1 receptor locus, design fluorescent dyes for specific labelling in complex tissue, and reveal ...
Julia Ast, Daniela Nasteska, Nicholas H. F. Fine, Daniel J. Nieves, Zsombor Koszegi, Yann Lanoiselée, Federica Cuozzo, Katrina Viloria, Andrea Bacon, Nguyet T. Luu, Philip N. Newsome, Davide Calebiro, Dylan M. Owen, Johannes Broichhagen, David J. Hodson   +14 more
doaj   +1 more source

Cluster analysis for localisation-based data sets: dos and don’ts when quantifying protein aggregates

Frontiers in Bioinformatics, 2023
Many proteins display a non-random distribution on the cell surface. From dimers to nanoscale clusters to large, micron-scale aggregations, these distributions regulate protein-protein interactions and signalling.
Luca Panconi, Dylan M. Owen, Juliette Griffié   +2 more
doaj   +1 more source

Clinical applications of exosome membrane proteins

Precision Clinical Medicine, 2020
Extracellular vesicles (EVs) are small membranous particles that can mediate cell-to-cell communication and which are divided into at least three categories according to their subcellular origin and size: exosomes, microvesicles, and apoptotic bodies ...
Qian Hu, Hang Su, Juan Li, Christopher J. Lyon, Wenfu Tang, Meihua Wan, Tony Y. Hu   +6 more
semanticscholar   +1 more source

Functional solubilization of the β2-adrenoceptor using diisobutylene maleic acid

iScience, 2021
Summary: The β2-adrenoceptor (β2AR) is a well-established target in asthma and a prototypical G protein-coupled receptor for biophysical studies. Solubilization of membrane proteins has classically involved the use of detergents.
Clare.R. Harwood, David A. Sykes, Bradley L. Hoare, Franziska M. Heydenreich, Romez Uddin, David R. Poyner, Stephen J. Briddon, D.B. Veprintsev   +7 more
doaj   +1 more source

Development of a membrane-based Gi-CASE biosensor assay for profiling compounds at cannabinoid receptors

Frontiers in Pharmacology, 2023
Introduction: The cannabinoid receptor (CBR) subtypes 1 (CB1R) and 2 (CB2R) are key components of the endocannabinoid system (ECS), playing a central role in the control of peripheral pain, inflammation and the immune response, with further roles in the ...
Morgan Scott-Dennis, Morgan Scott-Dennis, Fikri A. Rafani, Fikri A. Rafani, Yicheng Yi, Yicheng Yi, Themiya Perera, Themiya Perera, Clare R. Harwood, Clare R. Harwood, Wolfgang Guba, Arne C. Rufer, Uwe Grether, Dmitry B. Veprintsev, Dmitry B. Veprintsev, Dmitry B. Veprintsev, David A. Sykes, David A. Sykes, David A. Sykes   +18 more
doaj   +1 more source