Results 1 to 10 of about 9,896,950 (388)
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 +13 more
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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 +5 more
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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 +14 more
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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 +2 more
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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 +2 more
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Allostery in membrane proteins [PDF]
Current Opinion in Structural Biology, 2020 Membrane proteins are an integral part of signal transduction. To signal, membrane proteins must interact with a variety of lipid species, effectors, and other proteins in the biological membrane leading to an immense number of possible interactions. Despite this inherent complexity, accurate control of signaling must take place.
Cournia, Zoe, Chatzigoulas, Alexios
openaire +3 more sources
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 +2 more
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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 +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 +7 more
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Native Mass Spectrometry of Membrane Proteins.
Analytical Chemistry, 2020 Graphical Abstract Biological membranes formed of amphipathic lipid bilayers provide chemical barriers to separate cells from their external environments and define subcellular compartments.
J. Keener, Guozhi Zhang, M. Marty
semanticscholar +1 more source