Results 1 to 10 of about 1,639,954 (343)

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

open access: yesPharmacology 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
doaj   +1 more source

Exploring the kinetic selectivity of drugs targeting the β1‐adrenoceptor

open access: yesPharmacology 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
doaj   +1 more source

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

open access: yesNature 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
doaj   +1 more source

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

open access: yesFrontiers 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
doaj   +1 more source

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

open access: yesInternational 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
doaj   +1 more source

Physical limits to membrane curvature sensing by a single protein [PDF]

open access: yesPhys. Rev. E 108, 064407 (2023), 2022
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

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

open access: yesFrontiers 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   +18 more
doaj   +1 more source

Allostery in membrane proteins [PDF]

open access: yesCurrent 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.
Zoe Cournia, Alexios Chatzigoulas
openaire   +3 more sources

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

open access: yesFrontiers 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   +5 more
doaj   +1 more source

In vitro reconstitution of substrate S-acylation by the zDHHC family of protein acyltransferases

open access: yesOpen Biology, 2022
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
doaj   +1 more source

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