Results 1 to 10 of about 1,639,954 (343)
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
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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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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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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Abstract P-40: Computational Evaluation of Binding of Heme-Focused Library to Cholesterol-Metabolizing P450 Enzymes from Mycobacterium tuberculosis [PDF]
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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Physical limits to membrane curvature sensing by a single protein [PDF]
Membrane curvature sensing is essential for a diverse range of biological processes. Recent experiments have revealed that a single nanometer-sized septin protein can distinguish between membrane-coated glass beads of one micron and three micron diameters, even though the septin is orders of magnitude smaller than the beads.
arxiv +1 more source
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+18 more
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Allostery in membrane proteins [PDF]
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.
Zoe Cournia, Alexios Chatzigoulas
openaire +3 more sources
Super-Resolution Imaging Approaches for Quantifying F-Actin in Immune Cells
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+5 more
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In vitro reconstitution of substrate S-acylation by the zDHHC family of protein acyltransferases
Protein S-acylation, more commonly known as protein palmitoylation, is a biological process defined by the covalent attachment of long chain fatty acids onto cysteine residues of a protein, effectively altering the local hydrophobicity and influencing ...
R. Elliot Murphy, Anirban Banerjee
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