Rational design of dualsteric GPCR ligands: quests and promise.
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Drugs for allosteric sites on receptorsNovel Allosteric Modulators of G Protein-coupled ReceptorsA new mechanism of allostery in a G protein-coupled receptor dimerMapping the druggable allosteric space of G-protein coupled receptors: a fragment-based molecular dynamics approach.Design strategies for bivalent ligands targeting GPCRs.Allosteric Modulation: An Alternate Approach Targeting the Cannabinoid CB1 Receptor.Allosteric modulation of purine and pyrimidine receptors.Molecular determinants of selectivity and efficacy at the dopamine D3 receptor.Agonists with supraphysiological efficacy at the muscarinic M2 ACh receptor.Muscarinic receptors as model targets and antitargets for structure-based ligand discovery.Separation of on-target efficacy from adverse effects through rational design of a bitopic adenosine receptor agonistMolecular alliance-from orthosteric and allosteric ligands to dualsteric/bitopic agonists at G protein coupled receptors.Biased agonism at G protein-coupled receptors: the promise and the challenges--a medicinal chemistry perspective.Muscarinic acetylcholine receptors: novel opportunities for drug development.Rational Modification of the Biological Profile of GPCR Ligands through Combination with Other Biologically Active Moieties.On the 'micro'-pharmacodynamic and pharmacokinetic mechanisms that contribute to long-lasting drug action.On the different experimental manifestations of two-state 'induced-fit' binding of drugs to their cellular targetsCell membranes… and how long drugs may exert beneficial pharmacological activity in vivoMultivalent approaches and beyond: novel tools for the investigation of dopamine D2 receptor pharmacology.Pharmacologically distinct phenotypes of α1B -adrenoceptors: variation in binding and functional affinities for antagonists.A structural chemogenomics analysis of aminergic GPCRs: lessons for histamine receptor ligand design.Modeling Complexes of Transmembrane Proteins: Systematic Analysis of ProteinProtein Docking Tools.'Partial' competition of heterobivalent ligand binding may be mistaken for allosteric interactions: a comparison of different target interaction models.Molecular pharmacology of G protein-coupled receptors. Editorial.Avidity and positive allosteric modulation/cooperativity act hand in hand to increase the residence time of bivalent receptor ligands.Simplified models for heterobivalent ligand binding: when are they applicable and which are the factors that affect their target residence time.Synthesis and Pharmacological Characterization of Novel trans-Cyclopropylmethyl-Linked Bivalent Ligands That Exhibit Selectivity and Allosteric Pharmacology at the Dopamine D3 Receptor (D3R).NPYFa, A Chimeric Peptide of Met-Enkephalin, and NPFF Induces Tolerance-Free Analgesia.Dopamine D2 receptors dimers: how can we pharmacologically target them?Heterodimerization of Dibenzodiazepinone-Type Muscarinic Acetylcholine Receptor Ligands Leads to Increased M2R Affinity and Selectivity.Link between a high for drug binding and a fast clinical action: to be or not to be?M1 muscarinic cetylcholine receptor allosteric modulators as potential therapeutic opportunities for treating Alzheimer's disease
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P2860
Rational design of dualsteric GPCR ligands: quests and promise.
description
article científic
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article scientifique
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articolo scientifico
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artigo científico
@pt
bilimsel makale
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scientific article published on 05 February 2010
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vedecký článok
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vetenskaplig artikel
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videnskabelig artikel
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vědecký článek
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name
Rational design of dualsteric GPCR ligands: quests and promise.
@en
Rational design of dualsteric GPCR ligands: quests and promise.
@nl
type
label
Rational design of dualsteric GPCR ligands: quests and promise.
@en
Rational design of dualsteric GPCR ligands: quests and promise.
@nl
prefLabel
Rational design of dualsteric GPCR ligands: quests and promise.
@en
Rational design of dualsteric GPCR ligands: quests and promise.
@nl
P2093
P2860
P1476
Rational design of dualsteric GPCR ligands: quests and promise.
@en
P2093
Christian Tränkle
Elisabetta Barocelli
Evi Kostenis
Klaus Mohr
P2860
P304
P356
10.1111/J.1476-5381.2009.00601.X
P407
P577
2010-02-05T00:00:00Z