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

A universal homogeneous assay for high-throughput determination of binding kinetics

(2015) Felix Schiele et al.   ANALYTICAL BIOCHEMISTRY

Rational Modulation of the Induced-Fit Conformational Change for Slow-Onset Inhibition in Mycobacterium tuberculosis InhA

(2015) Cheng-Tsung Lai et al.   BIOCHEMISTRY

Design strategies to address kinetics of drug binding and residence time

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

Which trails are your drugs taking?

(2015) Rumin Zhang   Nature Chemical Biology

Translating slow-binding inhibition kinetics into cellular and in vivo effects

(2015) Grant K Walkup et al.   Nature Chemical Biology

Prolonged and tunable residence time using reversible covalent kinase inhibitors

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

A selective inhibitor of PRMT5 with in vivo and in vitro potency in MCL models

(2015) Elayne Chan-Penebre et al.   Nature Chemical Biology

Kinetics of protein–ligand unbinding: Predicting pathways, rates, and rate-limiting steps

(2015) Pratyush Tiwary et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Long Residence Time Inhibition of EZH2 in Activated Polycomb Repressive Complex 2

(2014) Glenn S. Van Aller et al.   ACS Chemical Biology

A Structural and Energetic Model for the Slow-Onset Inhibition of the Mycobacterium tuberculosis Enoyl-ACP Reductase InhA

(2014) Huei-Jiun Li et al.   ACS Chemical Biology

Pharmacokinetics and the drug–target residence time concept

(2013) Göran Dahl et al.   DRUG DISCOVERY TODAY

Structure-kinetic relationship study of CDK8/CycC specific compounds

(2013) E. V. Schneider et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

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

(2012) Dong Guo et al.   BRITISH JOURNAL OF PHARMACOLOGY

Conformational Adaptation Drives Potent, Selective and Durable Inhibition of the Human Protein Methyltransferase DOT1L

(2012) Aravind Basavapathruni et al.   Chemical Biology & Drug Design

Evidence for dynamics in proteins as a mechanism for ligand dissociation

(2012) Mary J Carroll et al.   Nature Chemical Biology

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

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

Conformational adaptation in drug–target interactions and residence time

(2011) Robert A Copeland   Future Medicinal Chemistry

Shielded Hydrogen Bonds as Structural Determinants of Binding Kinetics: Application in Drug Design

(2011) Peter Schmidtke et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

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

Hsp90 (Heat Shock Protein 90) Inhibitor Occupancy Is a Direct Determinant of Client Protein Degradation and Tumor Growth Arrestin Vivo

(2010) Bonnie Tillotson et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

A Slow, Tight Binding Inhibitor of InhA, the Enoyl-Acyl Carrier Protein Reductase fromMycobacterium tuberculosis

(2010) Sylvia R. Luckner et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Slow-Onset Inhibition of the FabI Enoyl Reductase fromFrancisella tularensis: Residence Time andin VivoActivity

(2009) Hao Lu et al.   ACS Chemical Biology

Potent Inhibitors of HIV-1 Integrase Display a Two-Step, Slow-Binding Inhibition Mechanism Which Is Absent in a Drug-Resistant T66I/M154I Mutant

(2009) Edward P. Garvey et al.   BIOCHEMISTRY

Structural biology contributions to tyrosine kinase drug discovery

(2009) Sandra W Cowan-Jacob et al.   CURRENT OPINION IN CELL BIOLOGY

Integrating surface plasmon resonance biosensor-based interaction kinetic analyses into the lead discovery and optimization process

(2009) U Helena Danielson   Future Medicinal Chemistry

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

(2008) Peter J. Tummino et al.   BIOCHEMISTRY

Enzymes with lid-gated active sites must operate by an induced fit mechanism instead of conformational selection

(2008) S. M. Sullivan et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA