Results 1 to 10 of about 1,959,579 (299)

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

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

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

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

Abstract P-40: Computational Evaluation of Binding of Heme-Focused Library to Cholesterol-Metabolizing P450 Enzymes from Mycobacterium tuberculosis [PDF]

International Journal of Biomedicine, 2019
Background: Tuberculosis (TB), caused by pathogenic bacteria Mycobacterium tuberculosis (MTb), is known to be among top-10 causes of death worldwide.
Egor Marin, Natallia Strushkevich, Valentin Borshchevskiy   +2 more
doaj   +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

Super-Resolution Imaging Approaches for Quantifying F-Actin in Immune Cells

Frontiers in Cell and Developmental Biology, 2021
Immune cells comprise a diverse set of cells that undergo a complex array of biological processes that must be tightly regulated. A key component of cellular machinery that achieves this is the cytoskeleton.
Evelyn Garlick, Evelyn Garlick, Steven G. Thomas, Steven G. Thomas, Dylan M. Owen, Dylan M. Owen   +5 more
doaj   +1 more source

Probing expression of E-selectin using CRISPR-Cas9-mediated tagging with HiBiT in human endothelial cells

iScience, 2023
Summary: E-selectin is expressed on endothelial cells in response to inflammatory cytokines and mediates leukocyte rolling and extravasation. However, studies have been hampered by lack of experimental approaches to monitor expression in real time in ...
Lydia Ogrodzinski, Simon Platt, Joelle Goulding, Cameron Alexander, Tracy D. Farr, Jeanette Woolard, Stephen J. Hill, Laura E. Kilpatrick   +7 more
doaj   +1 more source