Functional efficacy of adenosine A₂A receptor agonists is positively correlated to their receptor residence time
about
Chemical, target, and bioactive properties of allosteric modulationBeyond Membrane Protein Structure: Drug Discovery, Dynamics and Difficulties.Understanding ligand-receptor non-covalent binding kinetics using molecular modeling.Ligand-dependent activation and deactivation of the human adenosine A(2A) receptor.Structure-Based Design of Reactive Nucleosides for Site-Specific Modification of the A2A Adenosine ReceptorMolecular docking screening using agonist-bound GPCR structures: probing the A2A adenosine receptor.Insulin-increased L-arginine transport requires A(2A) adenosine receptors activation in human umbilical vein endothelium.Mass spectrometry-based ligand binding assays on adenosine A1 and A2A receptors.Adenosine A2A receptor agonists with potent antiplatelet activity.The role of kinetic context in apparent biased agonism at GPCRs.Computational analysis and predictive modeling of polymorph descriptors.Characterization of 12 GnRH peptide agonists - a kinetic perspectiveStructure-Activity Analysis of Biased Agonism at the Human Adenosine A3 Receptor.Label-free cell phenotypic assessment of the biased agonism and efficacy of agonists at the endogenous muscarinic M3 receptors.Label-free drug discovery.New concepts in pharmacological efficacy at 7TM receptors: IUPHAR review 2.Drug-target residence time--a case for G protein-coupled receptors.Biased agonism at G protein-coupled receptors: the promise and the challenges--a medicinal chemistry perspective.Scintillation proximity assay (SPA) as a new approach to determine a ligand's kinetic profile. A case in point for the adenosine A1 receptor.Combining label-free cell phenotypic profiling with computational approaches for novel drug discovery.Compound annotation with real time cellular activity profiles to improve drug discovery.Mechanistic models enable the rational use of in vitro drug-target binding kinetics for better drug effects in patients.The drug-target residence time model: a 10-year retrospective.Structure-Activity Relationships of the Sustained Effects of Adenosine A2A Receptor Agonists Driven by Slow Dissociation Kinetics.Advanced molecular dynamics simulation methods for kinase drug discovery.TSPO ligand residence time: a new parameter to predict compound neurosteroidogenic efficacy.Kv 11.1 (hERG)-induced cardiotoxicity: a molecular insight from a binding kinetics study of prototypical Kv 11.1 (hERG) inhibitors.Pharmacology and structure of isolated conformations of the adenosine A₂A receptor define ligand efficacy.Dual-point competition association assay: a fast and high-throughput kinetic screening method for assessing ligand-receptor binding kinetics.Protein conformational plasticity and complex ligand-binding kinetics explored by atomistic simulations and Markov models.A covalent antagonist for the human adenosine A2A receptor.Molecular mechanism of allosteric modulation at GPCRs: insight from a binding kinetics study at the human A1 adenosine receptor.Simplified models for heterobivalent ligand binding: when are they applicable and which are the factors that affect their target residence time.Binding Thermodynamics and Kinetics Calculations Using Chemical Host and Guest: A Comprehensive Picture of Molecular Recognition.Adaptive Multilevel Splitting Method for Molecular Dynamics Calculation of Benzamidine-Trypsin Dissociation Time.A binding kinetics study of human adenosine A3 receptor agonists.A kinetic view of GPCR allostery and biased agonism.Label-free NMR-based dissociation kinetics determination.Binding kinetics of ZM241385 derivatives at the human adenosine A2A receptor.A two-state model for the kinetics of competitive radioligand binding.
P2860
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P2860
Functional efficacy of adenosine A₂A receptor agonists is positively correlated to their receptor residence time
description
2012 nî lūn-bûn
@nan
2012年の論文
@ja
2012年論文
@yue
2012年論文
@zh-hant
2012年論文
@zh-hk
2012年論文
@zh-mo
2012年論文
@zh-tw
2012年论文
@wuu
2012年论文
@zh
2012年论文
@zh-cn
name
Functional efficacy of adenosi ...... their receptor residence time
@en
Functional efficacy of adenosi ...... their receptor residence time
@nl
type
label
Functional efficacy of adenosi ...... their receptor residence time
@en
Functional efficacy of adenosi ...... their receptor residence time
@nl
prefLabel
Functional efficacy of adenosi ...... their receptor residence time
@en
Functional efficacy of adenosi ...... their receptor residence time
@nl
P2860
P50
P1476
Functional efficacy of adenosi ...... their receptor residence time
@en
P2093
Thea Mulder-Krieger
P2860
P304
P356
10.1111/J.1476-5381.2012.01897.X
P407
P577
2012-07-01T00:00:00Z