Drug-target residence time--a case for G protein-coupled receptors (Q38189272)

30 August 2017

title

Drug-target residence time--a case for G protein-coupled receptors (English)

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G protein-coupled receptor

30 August 2017

main subject

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Dong Guo

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Laura H Heitman

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Adriaan P IJzerman

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Julia M Hillger

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30 August 2017

publication date

18 February 2014

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Medicinal Research Reviews

30 August 2017

published in

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30 August 2017

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30 August 2017

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30 August 2017

page(s)

856-892

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Drug-target residence time and its implications for lead optimization

30 August 2017

cites work

1 reference

Biochemical mechanisms of New Molecular Entities (NMEs) approved by United States FDA during 2001-2004: mechanisms leading to optimal efficacy and safety

21 January 2018

1 reference

How were new medicines discovered?

21 January 2018

1 reference

Biochemical mechanisms of drug action: what does it take for success?

21 January 2018

1 reference

Conformational adaptation in drug-target interactions and residence time

21 January 2018

1 reference

Long‐lasting target binding and rebinding as mechanisms to prolong in vivo drug action

21 January 2018

1 reference

Insurmountable AT(1) receptor antagonism: the need for different antagonist binding states of the receptor

21 January 2018

1 reference

A two-state receptor model for the interaction between angiotensin II type 1 receptors and non-peptide antagonists

21 January 2018

1 reference

Slow antagonist dissociation and long-lasting in vivo receptor protection

21 January 2018

1 reference

Binding kinetics and mechanism of action: toward the discovery and development of better and best in class drugs

21 January 2018

1 reference

Residence time of receptor-ligand complexes and its effect on biological function

21 January 2018

1 reference

Pharmacokinetics and the drug-target residence time concept

21 January 2018

1 reference

Target-drug interactions: first principles and their application to drug discovery

21 January 2018

1 reference

Structure-kinetic relationships--an overlooked parameter in hit-to-lead optimization: a case of cyclopentylamines as chemokine receptor 2 antagonists

21 January 2018

1 reference

Structural optimization affording 2-(R)-(1-(R)-3, 5-bis(trifluoromethyl)phenylethoxy)-3-(S)-(4-fluoro)phenyl-4- (3-oxo-1,2,4-triazol-5-yl)methylmorpholine, a potent, orally active, long-acting morpholine acetal human NK-1 receptor antagonist

21 January 2018

1 reference

Characterization of aclidinium bromide, a novel inhaled muscarinic antagonist, with long duration of action and a favorable pharmacological profile.

21 January 2018

1 reference

A general method for the covalent labeling of fusion proteins with small molecules in vivo

21 January 2018

1 reference

Analytical method for simultaneously measuring ex vivo drug receptor occupancy and dissociation rate: application to (R)-dimethindene occupancy of central histamine H1 receptors.

21 January 2018

1 reference

Estimation of the dissociation rate of unlabelled ligand-receptor complexes by a 'two-step' competition binding approach

21 January 2018

1 reference

(-)-S-[3H]CGP-12177 and its use to determine the rate constants of unlabeled beta-adrenergic antagonists

21 January 2018

1 reference

Quantifying the association and dissociation rates of unlabelled antagonists at the muscarinic M3 receptor.

21 January 2018

1 reference

Pharmacological characterization of GSK1004723, a novel, long-acting antagonist at histamine H(1) and H(3) receptors

21 January 2018

1 reference

Functional efficacy of adenosine A₂A receptor agonists is positively correlated to their receptor residence time

21 January 2018

1 reference

Dual-point competition association assay: a fast and high-throughput kinetic screening method for assessing ligand-receptor binding kinetics

21 January 2018

1 reference

Clozapine, atypical antipsychotics, and the benefits of fast-off D2 dopamine receptor antagonism

21 January 2018

1 reference

Determining the potency and molecular mechanism of action of insurmountable antagonists

21 January 2018

1 reference

How can the differences among AT1-receptor antagonists be explained?

21 January 2018

1 reference

Distinctions between non-peptide angiotensin II AT1-receptor antagonists.

21 January 2018

1 reference

New insights in insurmountable antagonism

21 January 2018

1 reference

Models and methods for studying insurmountable antagonism

21 January 2018

1 reference

Kinetic versus allosteric mechanisms to explain insurmountable antagonism and delayed ligand dissociation

21 January 2018

1 reference

Higher-throughput, label-free, real-time molecular interaction analysis

21 January 2018

1 reference

Kinetic binding analysis of aptamers targeting HIV-1 proteins by a combination of a microbalance array and mass spectrometry (MAMS).

21 January 2018

1 reference

Surface acoustic wave sensors in the bioanalytical field: recent trends and challenges

21 January 2018

1 reference

Grading the commercial optical biosensor literature-Class of 2008: 'The Mighty Binders'.

21 January 2018

1 reference

Biophysical mapping of the adenosine A2A receptor

21 January 2018

1 reference

The properties of thermostabilised G protein-coupled receptors (StaRs) and their use in drug discovery.

21 January 2018

1 reference

Discovery of 1,2,4-Triazine Derivatives as Adenosine A 2A Antagonists using Structure Based Drug Design

21 January 2018

1 reference

Comprehensive repertoire and phylogenetic analysis of the G protein-coupled receptors in human and mouse

21 January 2018

1 reference

Seven-transmembrane receptors

21 January 2018

1 reference

How many drug targets are there?

21 January 2018

1 reference

The druggable genome: an update

21 January 2018

1 reference

An update of novel screening methods for GPCR in drug discovery

21 January 2018

1 reference

Novel P2Y12 adenosine diphosphate receptor antagonists for inhibition of platelet aggregation (II): pharmacodynamic and pharmacokinetic characterization

21 January 2018

1 reference

Axoplasmic transport and possible recycling of opiate receptors labelled with 3H-lofentanil

21 January 2018

1 reference

21 January 2018

1 reference

Molecular determinants of drug-receptor binding kinetics

21 January 2018

1 reference

Can the pharmaceutical industry reduce attrition rates?

21 January 2018

1 reference

Identification of a family of muscarinic acetylcholine receptor genes

21 January 2018

1 reference

The molecular basis of muscarinic receptor diversity

21 January 2018

1 reference

Molecular biology of muscarinic acetylcholine receptors

21 January 2018

1 reference

Global Strategy for the Diagnosis, Management, and Prevention of Chronic Obstructive Pulmonary Disease

21 January 2018

1 reference

Is a long-acting inhaled bronchodilator the first agent to use in stable chronic obstructive pulmonary disease?

21 January 2018

1 reference

Tiotropium (Spiriva): mechanistical considerations and clinical profile in obstructive lung disease

21 January 2018

1 reference

Ba 679 BR, a novel long-acting anticholinergic bronchodilator

21 January 2018

1 reference

Preclinical evaluation of long-acting muscarinic antagonists: comparison of tiotropium and investigational drugs.

21 January 2018

1 reference

The Influence of receptor kinetics on the onset and duration of action and the therapeutic index of NVA237 and tiotropium

21 January 2018

1 reference

Efficacy and safety of once-daily NVA237 in patients with moderate-to-severe COPD: the GLOW1 trial

21 January 2018

1 reference

Molecular basis for the long duration of action and kinetic selectivity of tiotropium for the muscarinic M3 receptor.

21 January 2018

1 reference

Structure and dynamics of the M3 muscarinic acetylcholine receptor

21 January 2018

1 reference

Design of drugs involving the concepts and theories of drug metabolism and pharmacokinetics

21 January 2018

1 reference

A 4-year trial of tiotropium in chronic obstructive pulmonary disease

21 January 2018

1 reference

Pharmacodynamic steady state of tiotropium in patients with chronic obstructive pulmonary disease

21 January 2018

1 reference

Discovery of novel quaternary ammonium derivatives of (3R)-quinuclidinol esters as potent and long-acting muscarinic antagonists with potential for minimal systemic exposure after inhaled administration: identification of (3R)-3-{[hydroxy(di-2-thien

21 January 2018

1 reference

Aclidinium Bromide: Clinical Benefit in Patients with Moderate to Severe COPD

21 January 2018

1 reference

A randomised, placebo- and active-controlled dose-finding study of aclidinium bromide administered twice a day in COPD patients

21 January 2018

1 reference

The potential for aclidinium bromide, a new anticholinergic, in the management of chronic obstructive pulmonary disease

21 January 2018

1 reference

Aclidinium bromide for the treatment of chronic obstructive pulmonary disease

21 January 2018

1 reference

Inhalation by design: novel tertiary amine muscarinic M₃ receptor antagonists with slow off-rate binding kinetics for inhaled once-daily treatment of chronic obstructive pulmonary disease.

21 January 2018

1 reference

Pharmacological characterization of the muscarinic receptor antagonist, glycopyrrolate, in human and guinea-pig airways

21 January 2018

1 reference

Exploring the mechanism of agonist efficacy: a relationship between efficacy and agonist dissociation rate at the muscarinic M3 receptor.

21 January 2018

1 reference

Partial agonism at the human alpha(2A)-autoreceptor: role of binding duration

21 January 2018

1 reference

The mammalian tachykinin ligand-receptor system: an emerging target for central neurological disorders

21 January 2018

1 reference

Tachykinins and tachykinin receptors: a growing family

21 January 2018

1 reference

Tachykinins and tachykinin receptors: structure and activity relationships

21 January 2018

1 reference

Neurokinin(1) receptor antagonists as potential antidepressants

21 January 2018

1 reference

Peripheral tachykinin receptors as potential therapeutic targets in visceral diseases

21 January 2018

1 reference

Tachykinin receptor antagonists in clinical trials

21 January 2018

1 reference

Neurokinin 1 receptor antagonists: correlation between in vitro receptor interaction and in vivo efficacy

21 January 2018

1 reference

Correlation of neurokinin (NK) 1 receptor occupancy in gerbil striatum with behavioral effects of NK1 antagonists

21 January 2018

1 reference

Characterization of RO4583298 as a novel potent, dual antagonist with in vivo activity at tachykinin NK₁ and NK₃ receptors

21 January 2018

1 reference

Characterization of the binding and activity of a high affinity, pseudoirreversible morpholino tachykinin NK1 receptor antagonist

21 January 2018

1 reference

Pyrrolidine-carboxamides and oxadiazoles as potent hNK1 antagonists

21 January 2018

1 reference

Fused bicyclic pyrrolizinones as new scaffolds for human NK1 antagonists

21 January 2018

1 reference

Substituted fused bicyclic pyrrolizinones as potent, orally bioavailable hNK1 antagonists.

21 January 2018

1 reference

Fused tricyclic pyrrolizinones that exhibit pseudo-irreversible blockade of the NK1 receptor

21 January 2018

1 reference

Discovery process and pharmacological characterization of 2-(S)-(4-fluoro-2-methylphenyl)piperazine-1-carboxylic acid [1-(R)-(3,5-bis-trifluoromethylphenyl)ethyl]methylamide (vestipitant) as a potent, selective, and orally active NK1 receptor antago

21 January 2018

1 reference

Discovery and biological characterization of (2R,4S)-1'-acetyl-N-{(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethyl}-2-(4-fluoro-2-methylphenyl)-N-methyl-4,4'-bipiperidine-1-carboxamide as a new potent and selective neurokinin 1 (NK1) receptor antagonist

21 January 2018

1 reference

3,4-Dihydroxyphenylalanine and 5-hydroxytryptophan as reserpine antagonists

21 January 2018

1 reference

Dopamine receptors for every species: gene duplications and functional diversification in Craniates

21 January 2018

1 reference

What has been learnt from study of dopamine receptors in Parkinson's disease?

21 January 2018

1 reference

Low dopamine D(2) receptor binding potential in social phobia

21 January 2018

1 reference

Dopamine and the diseased brain

21 January 2018

1 reference

The nigrostriatal DA pathway and Parkinson's disease

21 January 2018

1 reference

Relationship between functional dopamine D2 and D3 receptors gene polymorphisms and neuroleptic malignant syndrome

21 January 2018

1 reference

D1 dopamine receptor: a putative neurochemical and behavioral link to cocaine action

21 January 2018

1 reference

Dopamine supersensitivity correlates with D2High states, implying many paths to psychosis

21 January 2018

1 reference

Treatments for schizophrenia: a critical review of pharmacology and mechanisms of action of antipsychotic drugs

21 January 2018

1 reference

Pharmacology of JNJ-37822681, a specific and fast-dissociating D2 antagonist for the treatment of schizophrenia

21 January 2018

1 reference

Multiple Dopamine Functions at Different Time Courses

21 January 2018

1 reference

Effects of clozapine on cerebral catecholaminergic neurone systems

21 January 2018

1 reference

Does fast dissociation from the dopamine d(2) receptor explain the action of atypical antipsychotics?: A new hypothesis

21 January 2018

1 reference

A double-blind, randomized, placebo-controlled study with JNJ-37822681, a novel, highly selective, fast dissociating D₂ receptor antagonist in the treatment of acute exacerbation of schizophrenia

21 January 2018

1 reference

Characterization of a 41-Residue Ovine Hypothalamic Peptide That Stimulates Secretion of Corticotropin and β-Endorphin

21 January 2018

1 reference

The CRF peptide family and their receptors: yet more partners discovered

21 January 2018

1 reference

CRF and CRF receptors: role in stress responsivity and other behaviors

21 January 2018

1 reference

CP-154,526: a potent and selective nonpeptide antagonist of corticotropin releasing factor receptors.

21 January 2018

1 reference

The corticotropin-releasing factor receptor: a novel target for the treatment of depression and anxiety-related disorders

21 January 2018

1 reference

The corticosteroid receptor hypothesis of depression

21 January 2018

1 reference

Recent advances in small molecule antagonists of the corticotropin-releasing factor type-1 receptor-focus on pharmacology and pharmacokinetics

21 January 2018

1 reference

Binding kinetics redefine the antagonist pharmacology of the corticotropin-releasing factor type 1 receptor.

21 January 2018

1 reference

Quantitative pharmacological analysis of antagonist binding kinetics at CRF1 receptors in vitro and in vivo

21 January 2018

1 reference

Corticotropin releasing factor (CRF) receptor modulators: progress and opportunities for new therapeutic agents

21 January 2018

1 reference

Non-peptidic CRF1 receptor antagonists for the treatment of anxiety, depression and stress disorders

21 January 2018

1 reference

Structure of class B GPCR corticotropin-releasing factor receptor 1

21 January 2018

1 reference

Non-peptide corticotropin-releasing hormone antagonists: syntheses and structure-activity relationships of 2-anilinopyrimidines and -triazines

21 January 2018

1 reference

Risperidone irreversibly binds to and inactivates the h5-HT7 serotonin receptor

21 January 2018

1 reference

Bopindolol is a slowly dissociating beta 1-adrenoceptor antagonist when compared to other beta-blockers

21 January 2018

1 reference

Functional and Biochemical Rationales for the 24-Hour-Long Duration of Action of Olodaterol

21 January 2018

1 reference

The CCR5 receptor-based mechanism of action of 873140, a potent allosteric noncompetitive HIV entry inhibitor

21 January 2018

1 reference

Pharmacological characterization of Sch527123, a potent allosteric CXCR1/CXCR2 antagonist

21 January 2018

1 reference

Kinetics of nonpeptide antagonist binding to the human gonadotropin-releasing hormone receptor: Implications for structure-activity relationships and insurmountable antagonism

21 January 2018

1 reference

Biochemical characterization of desloratadine, a potent antagonist of the human histamine H(1) receptor

21 January 2018

1 reference

Multifaceted approach to determine the antagonist molecular mechanism and interaction of ibodutant ([1-(2-phenyl-1R-[[1-(tetrahydropyran-4-ylmethyl)-piperidin-4-ylmethyl]-carbamoyl]-ethylcarbamoyl)-cyclopentyl]-amide) at the human tachykinin NK2 rec

21 January 2018

1 reference

Identification of a critical residue in the transmembrane domain 2 of tachykinin neurokinin 3 receptor affecting the dissociation kinetics and antagonism mode of osanetant (SR 142801) and piperidine-based structures

21 January 2018

1 reference

Binding kinetics differentiates functional antagonism of orexin-2 receptor ligands

21 January 2018

1 reference

GSK1562590, a slowly dissociating urotensin-II receptor antagonist, exhibits prolonged pharmacodynamic activity ex vivo

21 January 2018

1 reference

Identification and characterization of pseudoirreversible nonpeptide antagonists of the neuropeptide Y Y5 receptor and development of a novel Y5-selective radioligand

21 January 2018

1 reference

A clinical trial assessing the safety and efficacy of taranabant, a CB1R inverse agonist, in obese and overweight patients: a high-dose study

21 January 2018

1 reference

A one-year study to assess the safety and efficacy of the CB1R inverse agonist taranabant in overweight and obese patients with type 2 diabetes

21 January 2018

1 reference

Gonadotropin-releasing-hormone-receptor antagonists

21 January 2018

1 reference

Efficacy and safety of twice-daily aclidinium bromide in COPD patients: the ATTAIN study

21 January 2018

1 reference

21 January 2018

Identifiers

DOI

10.1002/MED.21307

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30 August 2017

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