On the different experimental manifestations of two-state ‘induced-fit’ binding of drugs to their cellular targets

NanoBRET—A Novel BRET Platform for the Analysis of Protein–Protein Interactions

(2015) Thomas Machleidt et al.   ACS Chemical Biology

A universal homogeneous assay for high-throughput determination of binding kinetics

(2015) Felix Schiele et al.   ANALYTICAL BIOCHEMISTRY

Design strategies to address kinetics of drug binding and residence time

(2015) Kevin P. Cusack et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

‘Partial’ competition of heterobivalent ligand binding may be mistaken for allosteric interactions: a comparison of different target interaction models

(2015) Georges Vauquelin et al.   BRITISH JOURNAL OF PHARMACOLOGY

The Concise Guide to PHARMACOLOGY 2015/16: G protein-coupled receptors

(2015) Stephen PH Alexander et al.   BRITISH JOURNAL OF PHARMACOLOGY

Application of BRET to monitor ligand binding to GPCRs

(2015) Leigh A Stoddart et al.   NATURE METHODS

Using ancient protein kinases to unravel a modern cancer drug's mechanism

(2015) C. Wilson et al.   SCIENCE

A study of the molecular mechanism of binding kinetics and long residence times of human CCR5 receptor small molecule allosteric ligands

(2014) David C Swinney et al.   BRITISH JOURNAL OF PHARMACOLOGY

Surface plasmon resonance spectroscopy for characterisation of membrane protein–ligand interactions and its potential for drug discovery

(2013) Simon G. Patching   BIOCHIMICA ET BIOPHYSICA ACTA-BIOMEMBRANES

Exploring avidity: understanding the potential gains in functional affinity and target residence time of bivalent and heterobivalent ligands

(2013) Georges Vauquelin et al.   BRITISH JOURNAL OF PHARMACOLOGY

Pharmacokinetics and the drug–target residence time concept

(2013) Göran Dahl et al.   DRUG DISCOVERY TODAY

Avidity and positive allosteric modulation/cooperativity act hand in hand to increase the residence time of bivalent receptor ligands

(2013) Georges Vauquelin et al.   FUNDAMENTAL & CLINICAL PHARMACOLOGY

Hybrid Bombesin Analogues: Combining an Agonist and an Antagonist in Defined Distances for Optimized Tumor Targeting

(2013) Carsten Kroll et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

A comprehensive analysis of the influence of drug binding kinetics on drug action at molecular and systems levels

(2013) Ning Yin et al.   Molecular BioSystems

Activation and allosteric modulation of a muscarinic acetylcholine receptor

(2013) Andrew C. Kruse et al.   NATURE

Simplified models for heterobivalent ligand binding: when are they applicable and which are the factors that affect their target residence time

(2013) Georges Vauquelin   NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY

The IUPHAR/BPS Guide to PHARMACOLOGY: an expert-driven knowledgebase of drug targets and their ligands

(2013) Adam J. Pawson et al.   NUCLEIC ACIDS RESEARCH

Structure of the CCR5 Chemokine Receptor-HIV Entry Inhibitor Maraviroc Complex

(2013) Q. Tan et al.   SCIENCE

Radioligand dissociation measurements: potential interference of rebinding and allosteric mechanisms and physiological relevance of the biological model systems

(2012) Georges Vauquelin et al.   Expert Opinion on Drug Discovery

Label-free measuring and mapping of binding kinetics of membrane proteins in single living cells

(2012) Wei Wang et al.   Nature Chemistry

'Self-healing' dyes: intramolecular stabilization of organic fluorophores

(2012) Philip Tinnefeld et al.   NATURE METHODS

Bridging the gap: bitopic ligands of G-protein-coupled receptors

(2012) J. Robert Lane et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Determination of drug–receptor residence times by radioligand binding and functional assays: experimental strategies and physiological relevance

(2012) Georges Vauquelin   MedChemComm

The Best of Both Worlds? Bitopic Orthosteric/Allosteric Ligands of G Protein–Coupled Receptors

(2011) Celine Valant et al.   Annual Review of Pharmacology and Toxicology

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

(2011) Sara Núñez et al.   DRUG DISCOVERY TODAY

Conformational adaptation in drug–target interactions and residence time

(2011) Robert A Copeland   Future Medicinal Chemistry

Allosteric Model of Maraviroc Binding to CC Chemokine Receptor 5 (CCR5)

(2011) Javier Garcia-Perez et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Pathway and mechanism of drug binding to G-protein-coupled receptors

(2011) Ron O. Dror et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Rational design of dualsteric GPCR ligands: quests and promise

(2010) Klaus Mohr et al.   BRITISH JOURNAL OF PHARMACOLOGY

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

(2010) Georges Vauquelin et al.   BRITISH JOURNAL OF PHARMACOLOGY

Ligand binding assays at equilibrium: validation and interpretation

(2010) Edward C. Hulme et al.   BRITISH JOURNAL OF PHARMACOLOGY

Drug–target residence time: critical information for lead optimization

(2010) Hao Lu et al.   CURRENT OPINION IN CHEMICAL BIOLOGY

The dynamics of drug-target interactions: drug-target residence time and its impact on efficacy and safety

(2010) Robert A Copeland   Expert Opinion on Drug Discovery

New Insights into the Mechanisms whereby Low Molecular Weight CCR5 Ligands Inhibit HIV-1 Infection

(2010) Javier Garcia-Perez et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

In Vitro Antagonistic Properties of a New Angiotensin Type 1 Receptor Blocker, Azilsartan, in Receptor Binding and Function Studies

(2010) M. Ojima et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

On the mechanism of the persistent action of salmeterol: what is the current position?

(2009) RA Coleman   BRITISH JOURNAL OF PHARMACOLOGY

Affinity and Avidity in Antibody-Based Tumor Targeting

(2009) Stephen I. Rudnick et al.   CANCER BIOTHERAPY AND RADIOPHARMACEUTICALS

Binding sites of valsartan, candesartan and losartan with angiotensin II receptor 1 subtype by molecular modeling

(2009) Mohiuddin Ahmed Bhuiyan et al.   LIFE SCIENCES

Cellular assays as portals to seven-transmembrane receptor-based drug discovery

(2009) Terry P. Kenakin   NATURE REVIEWS DRUG DISCOVERY

Residence Time of Receptor−Ligand Complexes and Its Effect on Biological Function

(2008) Peter J. Tummino et al.   BIOCHEMISTRY

Involvement of the Second Extracellular Loop and Transmembrane Residues of CCR5 in Inhibitor Binding and HIV-1 Fusion: Insights into the Mechanism of Allosteric Inhibition

(2008) Kenji Maeda et al.   JOURNAL OF MOLECULAR BIOLOGY

Sartan–AT1 receptor interactions: In vitro evidence for insurmountable antagonism and inverse agonism

(2008) I. Van Liefde et al.   MOLECULAR AND CELLULAR ENDOCRINOLOGY

The Relative Activity of "Function Sparing" HIV-1 Entry Inhibitors on Viral Entry and CCR5 Internalization: Is Allosteric Functional Selectivity a Valuable Therapeutic Property?

(2008) V. M. Muniz-Medina et al.   MOLECULAR PHARMACOLOGY

Molecular characterisation of the interactions between olmesartan and telmisartan and the human angiotensin II AT1 receptor

(2007) M T Le et al.   BRITISH JOURNAL OF PHARMACOLOGY