Effects of target binding kinetics onin vivodrug efficacy: koff, konand rebinding

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

(2016) Georges Vauquelin et al.   BRITISH JOURNAL OF PHARMACOLOGY

Design strategies to address kinetics of drug binding and residence time

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

The Role of Binding Kinetics in GPCR Drug Discovery

(2015) David Swinney et al.   CURRENT TOPICS IN MEDICINAL CHEMISTRY

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

(2015) Georges Vauquelin   Expert Opinion on Drug Discovery

Which trails are your drugs taking?

(2015) Rumin Zhang   Nature Chemical Biology

Prolonged and tunable residence time using reversible covalent kinase inhibitors

(2015) J Michael Bradshaw et al.   Nature Chemical Biology

The drug–target residence time model: a 10-year retrospective

(2015) Robert A. Copeland   NATURE REVIEWS DRUG DISCOVERY

Target engagement and drug residence time can be observed in living cells with BRET

(2015) Matthew B. Robers et al.   Nature Communications

Pharmacokinetics and the drug–target residence time concept

(2013) Göran Dahl et al.   DRUG DISCOVERY TODAY

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

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

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

(2012) Georges Vauquelin   MedChemComm

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

(2011) Sara Núñez et al.   DRUG DISCOVERY TODAY

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

Influence of kinetics of drug binding on EGFR signaling: A comparative study of three EGFR signaling pathway models

(2011) Sneha Bairy et al.   PROTEINS-STRUCTURE FUNCTION AND BIOINFORMATICS

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

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

The effect of plasma protein binding on in vivo efficacy: misconceptions in drug discovery

(2010) Dennis A. Smith et al.   NATURE REVIEWS DRUG DISCOVERY

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

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

Early integration of pharmacokinetic and dynamic reasoning is essential for optimal development of lead compounds: strategic considerations

(2009) Johan Gabrielsson et al.   DRUG DISCOVERY TODAY

Ligands, their receptors and … plasma membranes

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

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

(2008) Peter J. Tummino et al.   BIOCHEMISTRY

Mechanism-based pharmacokinetic-pharmacodynamic (PK-PD) modeling in translational drug research

(2008) M DANHOF et al.   TRENDS IN PHARMACOLOGICAL SCIENCES