Mechanistic analysis of the function of agonists and allosteric modulators: reconciling two‐state and operational models

No abstract is available for this paper.

• Publication year

  2013

• Venue

  British Journal of Pharmacology

• Publication date

  2013-07-01

• Fields of study

  Medicine, Chemistry, Psychology

• Identifiers
  DOI 10.1111/bph.12231PMID 23647200PMCID PMC3831701
• External record

  Open on Semantic Scholar

• Source metadata

  Semantic Scholar, PubMed

• No claims are published for this paper.

• No concepts are published for this paper.

• R: A language and environment for statistical computing.

  2014cited by this paper
• Multiple active receptor conformation, agonist efficacy and maximum effect of the system: the conformation-based operational model of agonism.

  2013cited by this paper
• Application of receptor theory to allosteric modulation of receptors.

  2013cited by this paper
• Development of operational models of receptor activation including constitutive receptor activity and their use to determine the efficacy of the chemokine CCL17 at the CC chemokine receptor CCR4

  2012influential reference
• Allosteric modulation of seven transmembrane spanning receptors: theory, practice, and opportunities for central nervous system drug discovery.

  2012influential reference
• Biased signalling and allosteric machines: new vistas and challenges for drug discovery

  2012cited by this paper
• A simple method for quantifying functional selectivity and agonist bias.

  2012cited by this paper
• Stimulus Bias Provides Evidence for Conformational Constraints in the Structure of a G Protein-coupled Receptor*

  2012cited by this paper
• Quantifying Ligand Bias at Seven-Transmembrane Receptors

  2011cited by this paper
• Quantitative Analysis Reveals Multiple Mechanisms of Allosteric Modulation of the mGlu5 Receptor in Rat Astroglia

  2011cited by this paper
• Allosteric modulation of G protein-coupled receptors: a pharmacological perspective.

  2011cited by this paper
• A Monod-Wyman-Changeux Mechanism Can Explain G Protein-coupled Receptor (GPCR) Allosteric Modulation*

  2011cited by this paper
• Analysis of Agonism and Inverse Agonism in Functional Assays with Constitutive Activity: Estimation of Orthosteric Ligand Affinity Constants for Active and Inactive Receptor States

  2011cited by this paper
• How inverse can a neutral antagonist be? Strategic questions after the rimonabant issue.

  2010cited by this paper
• Seven Transmembrane Receptors as Shapeshifting Proteins: The Impact of Allosteric Modulation and Functional Selectivity on New Drug Discovery

  2010cited by this paper
• The asymmetric/symmetric activation of GPCR dimers as a possible mechanistic rationale for multiple signalling pathways.

  2010cited by this paper
• Systems biology: parameter estimation for biochemical models

  2009cited by this paper
• Allosteric Agonist Modulators

  2007cited by this paper
• Interaction of Novel Positive Allosteric Modulators of Metabotropic Glutamate Receptor 5 with the Negative Allosteric Antagonist Site Is Required for Potentiation of Receptor Responses

  2007cited by this paper
• Allosteric GPCR modulators: taking advantage of permissive receptor pharmacology.

  2007influential reference
• Assessing receptor affinity for inverse agonists: Schild and Cheng-Prusoff methods revisited.

  2007cited by this paper
• Predicting Dose-Response Curve Behavior: Mathematical Models of Allosteric Receptor-Ligand Interactions

  2006influential reference
• An Improved Differential Evolution Scheme for Noisy Optimization Problems

  2005influential reference
• New Concepts in Drug Discovery: Collateral Efficacy and Permissive Antagonism

  2005cited by this paper
• Allosteric Modulation of the Cannabinoid CB1 Receptor

  2005cited by this paper
• Analysis of Allosterism in Functional Assays

  2005cited by this paper
• Agonist induction, conformational selection, and mutant receptors

  2004cited by this paper
• Efficacy as a vector: the relative prevalence and paucity of inverse agonism.

  2004cited by this paper
• Assessing the (a)symmetry of concentration-effect curves: empirical versus mechanistic models.

  2002cited by this paper
• G Protein-Coupled Receptor Allosterism and Complexing

  2002cited by this paper
• Modeling the functional effects of allosteric modulators at pharmacological receptors: an extension of the two-state model of receptor activation.

  2000influential reference
• Differential Evolution – A Simple and Efficient Heuristic for global Optimization over Continuous Spaces

  1997cited by this paper
• The two-state model of receptor activation.

  1995cited by this paper
• An operational model of pharmacological agonism: the effect of E/[A] curve shape on agonist dissociation constant estimation

  1985cited by this paper
• Operational models of pharmacological agonism

  1983influential reference
• A ternary complex model explains the agonist-specific binding properties of the adenylate cyclase-coupled beta-adrenergic receptor.

  1980cited by this paper
• Inhibition of lysosomal plasminogen activator activity in experimental shock.

  1973cited by this paper
• The Relation between Classical and Cooperative Models for Drug Action

  1973cited by this paper
• On the analysis of pharmacological experiments in terms of an allosteric receptor model.

  1973cited by this paper
• On the application of "a plausible model" of allosteric proteins to the receptor for acetylcholine.

  1967cited by this paper
• ON THE NATURE OF ALLOSTERIC TRANSITIONS: A PLAUSIBLE MODEL.

  1965cited by this paper
• Interaction at end-plate receptors between different choline derivatives

  1957cited by this paper

• A mathematical formalism to quantify drug-target residence time.

  2025cites this paper
• Dalzanemdor (SAGE‐718), a novel, investigational N‐methyl‐D‐aspartate receptor positive allosteric modulator: Safety, tolerability, and clinical pharmacology in randomized dose‐finding studies in healthy participants and an open‐label study in participants with Huntington's disease

  2024cites this paper
• A 19F-qNMR-Guided Mathematical Model for G Protein-Coupled Receptor Signaling

  2023cites this paper
• Allosteric binding cooperativity in a kinetic context.

  2022cites this paper
• Therapeutic potential of allosteric modulators for the treatment of gastrointestinal motility disorders

  2022cites this paper
• Novel mathematical and computational models of G protein–coupled receptor signalling

  2021cites this paper
• Models for Lead Optimization

  2021cites this paper
• Recent Developments in Treating Cognitive Impairment Associated with Schizophrenia

  2021cites this paper
• Biased Allosteric Modulators: New Frontiers in GPCR Drug Discovery.

  2021cites this paper
• Analysis of the Function of Receptor Oligomers by Operational Models of Agonism

  2021cites this paper
• Involvement of the adenosine A1 receptor in the hypnotic effect of rosmarinic acid.

  2021cites this paper
• A Receptor Model With Binding Affinity, Activation Efficacy, and Signal Amplification Parameters for Complex Fractional Response Versus Occupancy Data

  2019cites this paper
• A mathematical model of parathyroid gland biology

  2019cites this paper
• Allosteric Modalities for Membrane-Bound Receptors: Insights from Drug Hunting for Brain Diseases.

  2019cites this paper
• Mathematical modeling of oligomerization and biased signaling of G-protein-coupled receptors

  2018cites this paper
• A method for the quantification of biased signalling at constitutively active receptors

  2018cites this paper
• New insight into isobolographic analysis for combinations of a full and partial agonist: Curved isoboles.

  2018cites this paper
• Quantifying the allosteric interactions within a G-protein-coupled receptor heterodimer.

  2018cites this paper
• Practical Strategies and Concepts in GPCR Allosteric Modulator Discovery: Recent Advances with Metabotropic Glutamate Receptors.

  2016cites this paper
• Quantitative Measure of Receptor Agonist and Modulator Equi-Response and Equi-Occupancy Selectivity

  2016cites this paper
• Bridging Model-Dependent Receptor Agonism and Allosterism Parameterization.

  2016cites this paper
• Operational models of allosteric modulation: caution is needed.

  2015cites this paper
• Investigation of the allosteric pharmacology of the 5-HT\(_3\) receptor identifying the potent allosteric modulator 5-chloroindole

  2015cites this paper
• Statistical framework for terminating evolutionary algorithms at their steady state

  2015cites this paper
• Quantitative analysis of receptor allosterism and its implication for drug discovery

  2015influential citation
• Farmacologia Bàsica Avançada

  2014cites this paper
• Exploring the Active Conformation of Cyclohexane Carboxylate Positive Allosteric Modulators of the Type 4 Metabotropic Glutamate Receptor

  2014cites this paper
• Estimation of ligand affinity constants for receptor states in functional studies involving the allosteric modulation of G protein-coupled receptors: implications for ligand bias.

  2014cites this paper