On the ‘micro’-pharmacodynamic and pharmacokinetic mechanisms that contribute to long-lasting drug action

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

Molecular mechanism of allosteric modulation at GPCRs: insight from a binding kinetics study at the human A1adenosine receptor

(2014) Dong Guo et al.   BRITISH JOURNAL OF PHARMACOLOGY

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

Drug-Target Residence Time-A Case for G Protein-Coupled Receptors

(2014) Dong Guo et al.   MEDICINAL RESEARCH REVIEWS

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

Phenotypic vs. Target-Based Drug Discovery for First-in-Class Medicines

(2013) D C Swinney   CLINICAL PHARMACOLOGY & THERAPEUTICS

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

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

Slow receptor dissociation is not a key factor in the duration of action of inhaled long-acting β2-adrenoceptor agonists

(2012) David A Sykes et al.   BRITISH JOURNAL OF PHARMACOLOGY

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

Crystal Structure of a Lipid G Protein-Coupled Receptor

(2012) M. A. Hanson et al.   SCIENCE

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

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

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

Comparative Biophysical Studies of Sartan Class Drug Molecules Losartan and Candesartan (CV-11974) with Membrane Bilayers

(2011) Charalambos Fotakis et al.   JOURNAL OF PHYSICAL CHEMISTRY B

How were new medicines discovered?

(2011) David C. Swinney et al.   NATURE REVIEWS DRUG DISCOVERY

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

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

(2010) A Packeu et al.   BRITISH JOURNAL OF PHARMACOLOGY

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

Nucleation

(2010) Peter G. Vekilov   CRYSTAL GROWTH & DESIGN

Drug–target residence time: critical information for lead optimization

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

Rebinding: or why drugs may act longerin vivothan expected from theirin vitrotarget residence time

(2010) Georges Vauquelin   Expert Opinion on Drug Discovery

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

A Lipid Pathway for Ligand Binding Is Necessary for a Cannabinoid G Protein-coupled Receptor

(2010) Dow P. Hurst et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Physics of protein–DNA interactions: mechanisms of facilitated target search

(2010) Anatoly B. Kolomeisky   PHYSICAL CHEMISTRY CHEMICAL PHYSICS

The reassertion profiles of long acting β2-adrenoceptor agonists in the guinea pig isolated trachea and human recombinant β2-adrenoceptor

(2010) S. Patel et al.   PULMONARY PHARMACOLOGY & THERAPEUTICS

Molecular mechanisms for the persistent bronchodilatory effect of the β2-adrenoceptor agonist salmeterol

(2009) A Szczuka et al.   BRITISH JOURNAL OF PHARMACOLOGY

Affinity and Avidity in Antibody-Based Tumor Targeting

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

Ligands, their receptors and … plasma membranes

(2009) G. Vauquelin et al.   MOLECULAR AND CELLULAR ENDOCRINOLOGY

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

(2009) Terry P. Kenakin   NATURE REVIEWS DRUG DISCOVERY

A Ligand Channel through the G Protein Coupled Receptor Opsin

(2009) Peter W. Hildebrand et al.   PLoS One

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

(2008) Peter J. Tummino et al.   BIOCHEMISTRY

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

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

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