Long-lasting target binding and rebinding as mechanisms to prolong in vivo drug action
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Slow receptor dissociation kinetics differentiate macitentan from other endothelin receptor antagonists in pulmonary arterial smooth muscle cellsTowards structural systems pharmacology to study complex diseases and personalized medicineInvestigational beta-2 adrenergic agonists for the treatment of chronic obstructive pulmonary disease.In vitro and in vivo pharmacological characterization of a neuropeptide S tetrabranched derivative.The ligand binding mechanism to purine nucleoside phosphorylase elucidated via molecular dynamics and machine learning.Receptor residence time trumps drug-likeness and oral bioavailability in determining efficacy of complement C5a antagonists.Discovery of inhibitors of insulin-regulated aminopeptidase as cognitive enhancers.Pharmacological characterization of tachykinin tetrabranched derivatives.Influence of emulsifiers on the characteristics of polyurethane structures used as drug carrier.Discovery of dual-action membrane-anchored modulators of incretin receptorsPharmacometric Models for Characterizing the Pharmacokinetics of Orally Inhaled Drugs.Spinal antinociceptive effects of the novel NOP receptor agonist PWT2-nociceptin/orphanin FQ in mice and monkeysThe experimental power of FR900359 to study Gq-regulated biological processes.An anti-TNF-α antibody mimetic to treat ocular inflammation.Clozapine, atypical antipsychotics, and the benefits of fast-off D2 dopamine receptor antagonism.Prediction of volume of distribution at steady state in humans: comparison of different approaches.Radioligand dissociation measurements: potential interference of rebinding and allosteric mechanisms and physiological relevance of the biological model systems.Ligand-receptor interaction platforms and their applications for drug discovery.Exploring avidity: understanding the potential gains in functional affinity and target residence time of bivalent and heterobivalent ligands.Relatively slow and long-lasting antimigraine effect of dihydroergotamine is most likely due to basic pharmacological attributes of the drug: a review.Drug-target residence time--a case for G protein-coupled receptors.Muscarinic receptor antagonists for the treatment of chronic obstructive pulmonary disease.Neuropeptides: metabolism to bioactive fragments and the pharmacology of their receptors.Umeclidinium bromide and vilanterol in combination for the treatment of chronic obstructive pulmonary disease.Update on ultra-long-acting β agonists in chronic obstructive pulmonary disease.On the 'micro'-pharmacodynamic and pharmacokinetic mechanisms that contribute to long-lasting drug action.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.On the different experimental manifestations of two-state 'induced-fit' binding of drugs to their cellular targetsStructure-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.Cell membranes… and how long drugs may exert beneficial pharmacological activity in vivoThe Role of Target Binding Kinetics in Drug Discovery.High performance enzyme kinetics of turnover, activation and inhibition for translational drug discovery.Drug-Target Kinetics in Drug Discovery.Use of a new proximity assay (NanoBRET) to investigate the ligand-binding characteristics of three fluorescent ligands to the human β1-adrenoceptor expressed in HEK-293 cells.'Partial' competition of heterobivalent ligand binding may be mistaken for allosteric interactions: a comparison of different target interaction models.Extrapyramidal side effects of antipsychotics are linked to their association kinetics at dopamine D2 receptors.[(3) H]UR-DE257: development of a tritium-labeled squaramide-type selective histamine H2 receptor antagonist.Negative cooperativity across β1-adrenoceptor homodimers provides insights into the nature of the secondary low-affinity CGP 12177 β1-adrenoceptor binding conformation.
P2860
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P2860
Long-lasting target binding and rebinding as mechanisms to prolong in vivo drug action
description
2010 nî lūn-bûn
@nan
2010 թուականի Հոկտեմբերին հրատարակուած գիտական յօդուած
@hyw
2010 թվականի հոտեմբերին հրատարակված գիտական հոդված
@hy
2010年の論文
@ja
2010年論文
@yue
2010年論文
@zh-hant
2010年論文
@zh-hk
2010年論文
@zh-mo
2010年論文
@zh-tw
2010年论文
@wuu
name
Long-lasting target binding and rebinding as mechanisms to prolong in vivo drug action
@ast
Long-lasting target binding and rebinding as mechanisms to prolong in vivo drug action
@en
Long-lasting target binding and rebinding as mechanisms to prolong in vivo drug action
@nl
type
label
Long-lasting target binding and rebinding as mechanisms to prolong in vivo drug action
@ast
Long-lasting target binding and rebinding as mechanisms to prolong in vivo drug action
@en
Long-lasting target binding and rebinding as mechanisms to prolong in vivo drug action
@nl
prefLabel
Long-lasting target binding and rebinding as mechanisms to prolong in vivo drug action
@ast
Long-lasting target binding and rebinding as mechanisms to prolong in vivo drug action
@en
Long-lasting target binding and rebinding as mechanisms to prolong in vivo drug action
@nl
P2860
P3181
P1476
Long-lasting target binding and rebinding as mechanisms to prolong in vivo drug action
@en
P2093
Georges Vauquelin
Steven J Charlton
P2860
P304
P3181
P356
10.1111/J.1476-5381.2010.00936.X
P407
P577
2010-10-01T00:00:00Z