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

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

(2012) RJ Slack et al.   BRITISH JOURNAL OF PHARMACOLOGY

Multiple active receptor conformation, agonist efficacy and maximum effect of the system: the conformation-based operational model of agonism

(2012) David Roche et al.   DRUG DISCOVERY TODAY

Stimulus Bias Provides Evidence for Conformational Constraints in the Structure of a G Protein-coupled Receptor

(2012) Karen J. Gregory et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

A Simple Method for Quantifying Functional Selectivity and Agonist Bias

(2011) Terry Kenakin et al.   ACS Chemical Neuroscience

Biased signalling and allosteric machines: new vistas and challenges for drug discovery

(2011) Terry P Kenakin   BRITISH JOURNAL OF PHARMACOLOGY

A Monod-Wyman-Changeux Mechanism Can Explain G Protein-coupled Receptor (GPCR) Allosteric Modulation

(2011) Meritxell Canals et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Allosteric Modulation of Seven Transmembrane Spanning Receptors: Theory, Practice, and Opportunities for Central Nervous System Drug Discovery

(2011) Bruce J. Melancon et al.   JOURNAL OF MEDICINAL CHEMISTRY

Analysis of Agonism and Inverse Agonism in Functional Assays with Constitutive Activity: Estimation of Orthosteric Ligand Affinity Constants for Active and Inactive Receptor States

(2011) F. J. Ehlert et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

Quantitative Analysis Reveals Multiple Mechanisms of Allosteric Modulation of the mGlu5 Receptor in Rat Astroglia

(2011) S. J. Bradley et al.   MOLECULAR PHARMACOLOGY

Quantifying Ligand Bias at Seven-Transmembrane Receptors

(2011) S. Rajagopal et al.   MOLECULAR PHARMACOLOGY

How inverse can a neutral antagonist be? Strategic questions after the rimonabant issue

(2010) Jesús Giraldo   DRUG DISCOVERY TODAY

Allosteric modulation of G protein-coupled receptors: A pharmacological perspective

(2010) Peter Keov et al.   NEUROPHARMACOLOGY

Seven Transmembrane Receptors as Shapeshifting Proteins: The Impact of Allosteric Modulation and Functional Selectivity on New Drug Discovery

(2010) T. Kenakin et al.   PHARMACOLOGICAL REVIEWS

Systems biology: parameter estimation for biochemical models

(2009) Maksat Ashyraliyev et al.   FEBS Journal

The asymmetric/symmetric activation of GPCR dimers as a possible mechanistic rationale for multiple signalling pathways

(2009) Xavier Rovira et al.   TRENDS IN PHARMACOLOGICAL SCIENCES