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

Lessons learned from the fate of AstraZeneca's drug pipeline: a five-dimensional framework

(2014) David Cook et al.   NATURE REVIEWS DRUG DISCOVERY

Overexpression of Pseudomonas aeruginosa LpxC with its inhibitors in an acrB-deficient Escherichia coli strain

(2014) Ning Gao et al.   PROTEIN EXPRESSION AND PURIFICATION

Discovery of Inhibitors of 4′-Phosphopantetheine Adenylyltransferase (PPAT) To Validate PPAT as a Target for Antibacterial Therapy

(2013) Boudewijn L. M. de Jonge et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Rational Optimization of Drug-Target Residence Time: Insights from Inhibitor Binding to the Staphylococcus aureus FabI Enzyme–Product Complex

(2013) Andrew Chang et al.   BIOCHEMISTRY

Exploring the UDP pocket of LpxC through amino acid analogs

(2013) Michael R. Hale et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Potent inhibition of DOT1L as treatment of MLL-fusion leukemia

(2013) S. R. Daigle et al.   BLOOD

Developing Irreversible Inhibitors of the Protein Kinase Cysteinome

(2013) Qingsong Liu et al.   CHEMISTRY & BIOLOGY

Pyridone Methylsulfone Hydroxamate LpxC Inhibitors for the Treatment of Serious Gram-Negative Infections

(2012) Justin I. Montgomery et al.   JOURNAL OF MEDICINAL CHEMISTRY

Impact of enzyme concentration and residence time on apparent activity recovery in jump dilution analysis

(2011) Robert A. Copeland et al.   ANALYTICAL BIOCHEMISTRY

Mechanisms DecreasingIn VitroSusceptibility to the LpxC Inhibitor CHIR-090 in the Gram-Negative Pathogen Pseudomonas aeruginosa

(2011) Ruth E. Caughlan et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Can the flow of medicines be improved? Fundamental pharmacokinetic and pharmacological principles toward improving Phase II survival

(2011) Paul Morgan et al.   DRUG DISCOVERY TODAY

Design and Synthesis of Inhaled p38 Inhibitors for the Treatment of Chronic Obstructive Pulmonary Disease

(2011) David S. Millan et al.   JOURNAL OF MEDICINAL CHEMISTRY

Phase II failures: 2008–2010

(2011) John Arrowsmith   NATURE REVIEWS DRUG DISCOVERY

Trends in Risks Associated With New Drug Development: Success Rates for Investigational Drugs

(2010) J A DiMasi et al.   CLINICAL PHARMACOLOGY & THERAPEUTICS

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

Systematic review and mixed treatment comparison of randomized evidence for empirical, pre-emptive and directed treatment strategies for invasive mould disease

(2010) N. Freemantle et al.   JOURNAL OF ANTIMICROBIAL CHEMOTHERAPY

Evaluation of the efficacy and safety of pamapimod, a p38 MAP kinase inhibitor, in a double-blind, methotrexate-controlled study of patients with active rheumatoid arthritis

(2009) Stanley B. Cohen et al.   ARTHRITIS AND RHEUMATISM

Selection between Michaelis–Menten and target-mediated drug disposition pharmacokinetic models

(2009) Xiaoyu Yan et al.   JOURNAL OF PHARMACOKINETICS AND PHARMACODYNAMICS

Absolute metabolite concentrations and implied enzyme active site occupancy in Escherichia coli

(2009) Bryson D Bennett et al.   Nature Chemical Biology

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

(2008) Peter J. Tummino et al.   BIOCHEMISTRY

Mechanism and Inhibition of LpxC: An Essential Zinc-Dependent Deacetylase of Bacterial Lipid A Synthesis

(2008) Pei Zhou et al.   CURRENT PHARMACEUTICAL BIOTECHNOLOGY