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

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

Functional efficacy of adenosine A2A receptor agonists is positively correlated to their receptor residence time

(2012) Dong Guo 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

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

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

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

Structural Basis of Allosteric Ligand-Receptor Interactions in the Insulin/Relaxin Peptide Family

(2009) Pierre De Meyts et al.   Annals of the New York Academy of Sciences

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

Exploring the Mechanism of Agonist Efficacy: A Relationship between Efficacy and Agonist Dissociation Rate at the Muscarinic M3 Receptor

(2009) D. A. Sykes et al.   MOLECULAR PHARMACOLOGY

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

(2008) Peter J. Tummino et al.   BIOCHEMISTRY