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

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

Insight into the molecular basis for the kinetic differences between the two insulin receptor isoforms

(2011) Louise Knudsen et al.   BIOCHEMICAL JOURNAL

Conformational adaptation in drug–target interactions and residence time

(2011) Robert A Copeland   Future Medicinal Chemistry

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

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

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

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

P.3.d.009 Pharmacology of JNJ-37822681, a specific and fast-dissociating D2 antagonist for the treatment of schizophrenia

(2010) X. Langlois et al.   EUROPEAN NEUROPSYCHOPHARMACOLOGY

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

Binding kinetics and mechanism of action: toward the discovery and development of better and best in class drugs

(2010) Rumin Zhang et al.   Expert Opinion on Drug Discovery

Binding properties of antagonists to Cannabinoid receptors in intact cells

(2010) Marie Wennerberg et al.   FUNDAMENTAL & CLINICAL PHARMACOLOGY

THRX-198321 Is a Bifunctional Muscarinic Receptor Antagonist and  2-Adrenoceptor Agonist (MABA) That Binds in a Bimodal and Multivalent Manner

(2010) T. Steinfeld et al.   MOLECULAR PHARMACOLOGY

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

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

Analytical method for simultaneously measuring ex vivo drug receptor occupancy and dissociation rate: Application to (R)-dimethindene occupancy of central histamine H1receptors

(2009) Siobhan Malany et al.   JOURNAL OF RECEPTORS AND SIGNAL TRANSDUCTION

Ligands, their receptors and … plasma membranes

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

Harmonic oscillator model of the insulin and IGF1 receptors’ allosteric binding and activation

(2009) Vladislav V Kiselyov et al.   Molecular Systems Biology

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

(2009) Terry P. Kenakin   NATURE REVIEWS DRUG DISCOVERY

Ligand binding and micro-switches in 7TM receptor structures

(2009) Rie Nygaard et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Antagonist-radioligand binding to D2L-receptors in intact cells

(2008) Ann Packeu et al.   BIOCHEMICAL PHARMACOLOGY

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

(2008) Peter J. Tummino et al.   BIOCHEMISTRY

Dimerization and oligomerization of G-protein-coupled receptors: debated structures with established and emerging functions

(2008) László Szidonya et al.   JOURNAL OF ENDOCRINOLOGY

Allosteric modulators of GPCRs: a novel approach for the treatment of CNS disorders

(2008) P. Jeffrey Conn et al.   NATURE REVIEWS DRUG DISCOVERY

The insulin receptor: a prototype for dimeric, allosteric membrane receptors?

(2008) Pierre De Meyts   TRENDS IN BIOCHEMICAL SCIENCES

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

Cooperative Binding of Insulin-Like Peptide 3 to a Dimeric Relaxin Family Peptide Receptor 2

(2007) Angela Manegold Svendsen et al.   ENDOCRINOLOGY