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

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

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

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

Clozapine, atypical antipsychotics, and the benefits of fast-off D2 dopamine receptor antagonism

(2012) Georges Vauquelin et al.   NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY

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

Association of Candesartan vs Losartan With All-Cause Mortality in Patients With Heart Failure

(2011) Maria Eklind-Cervenka   JAMA-JOURNAL OF THE AMERICAN MEDICAL ASSOCIATION

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

Elusive equilibrium: the challenge of interpreting receptor pharmacology using calcium assays

(2010) Steven J Charlton 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

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

Affinity and Avidity in Antibody-Based Tumor Targeting

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

Effects of losartan vs candesartan in reducing cardiovascular events in the primary treatment of hypertension

(2009) S E Kjeldsen et al.   JOURNAL OF HUMAN HYPERTENSION

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

(2008) Peter J. Tummino et al.   BIOCHEMISTRY