Drug-target residence time: critical information for lead optimization. - Test2 - elhamkhani - TriplyDB

Drug-target residence time: critical information for lead optimization.

Drug-target residence time: critical information for lead optimization.

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New agents for the treatment of drug-resistant Mycobacterium tuberculosis The application of tetracyclineregulated gene expression systems in the validation of novel drug targets in Mycobacterium tuberculosis A virtual screen discovers novel, fragment-sized inhibitors of Mycobacterium tuberculosis InhA Mechanism-based Inactivation by Aromatization of the Transaminase BioA Involved in Biotin Biosynthesis in Mycobaterium tuberculosis Evidence for dynamics in proteins as a mechanism for ligand dissociation Structure-kinetic relationship study of CDK8/CycC specific compounds Rational Optimization of Drug-Target Residence Time: Insights from Inhibitor Binding to the Staphylococcus aureus FabI Enzyme–Product Complex Structural Basis for the Recognition of Mycolic Acid Precursors by KasA, a Condensing Enzyme and Drug Target from Mycobacterium Tuberculosis Time-Dependent Diaryl Ether Inhibitors of InhA: Structure-Activity Relationship Studies of Enzyme Inhibition, Antibacterial Activity, and in vivo Efficacy Resistance Mechanisms and the Future of Bacterial Enoyl-Acyl Carrier Protein Reductase (FabI) Antibiotics Evaluating the sensitivity of Mycobacterium tuberculosis to biotin deprivation using regulated gene expression Drug discovery using chemical systems biology: weak inhibition of multiple kinases may contribute to the anti-cancer effect of nelfinavir Towards structural systems pharmacology to study complex diseases and personalized medicine P-loop conformation governed crizotinib resistance in G2032R-mutated ROS1 tyrosine kinase: clues from free energy landscape Synthesis and evaluation of chloramphenicol homodimers: molecular target, antimicrobial activity, and toxicity against human cells Slow-Onset Inhibition of Mycobacterium tuberculosis InhA: Revealing Molecular Determinants of Residence Time by MD Simulations A Four-Point Screening Method for Assessing Molecular Mechanism of Action (MMOA) Identifies Tideglusib as a Time-Dependent Inhibitor of Trypanosoma brucei GSK3β Endless Resistance. Endless Antibiotics?Noninvasive determination of 2-[18F]-fluoroisonicotinic acid hydrazide pharmacokinetics by positron emission tomography in Mycobacterium tuberculosis-infected mice Pathway and mechanism of drug binding to G-protein-coupled receptors.Examining the interactions of the splicing factor MBNL1 with target RNA sequences via a label-free, multiplex method The use of thermodynamic and kinetic data in drug discovery: decisive insight or increasing the puzzlement?Residence Times of Molecular Complexes in Solution from NMR Data of Intermolecular Hydrogen-Bond Scalar Coupling Potential strategies for increasing drug-discovery productivity.A quantitative mechanistic PK/PD model directly connects Btk target engagement and in vivo efficacy Understanding ligand-receptor non-covalent binding kinetics using molecular modeling.Mechanism of the Association Pathways for a Pair of Fast and Slow Binding Ligands of HIV-1 Protease.Multidimensional profiling of CSF1R screening hits and inhibitors: assessing cellular activity, target residence time, and selectivity in a higher throughput way.Rational Modulation of the Induced-Fit Conformational Change for Slow-Onset Inhibition in Mycobacterium tuberculosis InhA.Production and evaluation of an antimicrobial peptide-containing wafer formulation for topical application.Target engagement and drug residence time can be observed in living cells with BRET.Biomolecular Interactions of small-molecule inhibitors affecting the YopH protein tyrosine phosphatase.Receptor residence time trumps drug-likeness and oral bioavailability in determining efficacy of complement C5a antagonists.Mechanism and inhibition of the FabI enoyl-ACP reductase from Burkholderia pseudomallei Acyl protein thioesterase inhibitors as probes of dynamic S-palmitoylation.A spatiotemporal characterization of the effect of p53 phosphorylation on its interaction with MDM2.Targeting class I histone deacetylase 2 in MYC amplified group 3 medulloblastoma.Distinct ETA receptor binding mode of macitentan as determined by site directed mutagenesis Biosensor-based affinities and binding kinetics of small molecule antagonists to the adenosine A(2A) receptor reconstituted in HDL like particles.Evidence for Two Distinct Binding Sites for Lipoprotein Lipase on Glycosylphosphatidylinositol-anchored High Density Lipoprotein-binding Protein 1 (GPIHBP1).

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P2860

Drug-target residence time: critical information for lead optimization.

http://www.wikidata.org/entity/Q34054343

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2010 nî lūn-bûn

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2010 թուականի Յուլիսին հրատարակուած գիտական յօդուած

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2010 թվականի հուլիսին հրատարակված գիտական հոդված

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2010年の論文

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2010年論文

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2010年論文

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2010年論文

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2010年論文

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2010年論文

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2010年论文

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Drug-target residence time: critical information for lead optimization.

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Drug-target residence time: critical information for lead optimization.

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Drug-target residence time: critical information for lead optimization.

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Drug-target residence time: critical information for lead optimization.

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Drug-target residence time: critical information for lead optimization.

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J.CBPA.2010.06.176

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Current Opinion in Chemical Biology

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Drug-target residence time: critical information for lead optimization

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Hao Lu

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The isoniazid-NAD adduct is a slow, tight-binding inhibitor of InhA, the Mycobacterium tuberculosis enoyl reductase: adduct affinity and drug resistance

Slow Binding Inhibition and Mechanism of Resistance of Non-nucleoside Polymerase Inhibitors of Hepatitis C Virus

Structural basis and mechanism of enoyl reductase inhibition by triclosan

Slow-Onset Inhibition of the FabI Enoyl Reductase from Francisella tularensis : Residence Time and in Vivo Activity

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

Can the pharmaceutical industry reduce attrition rates?

Inhibitors of FabI, an enzyme drug target in the bacterial fatty acid biosynthesis pathway.

Update of KDBI: Kinetic Data of Bio-molecular Interaction database.

Slow onset inhibition of bacterial beta-ketoacyl-acyl carrier protein synthases by thiolactomycin.

Synthesis and kinetic analysis of some phosphonate analogs of cyclophostin as inhibitors of human acetylcholinesterase.

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