Drug-target residence time and its implications for lead optimization.
about
Thermodynamic analysis of Jun-Fos coiled coil peptide antagonistsLong-lasting target binding and rebinding as mechanisms to prolong in vivo drug actionA safe lithium mimetic for bipolar disorderLigand binding assays at equilibrium: validation and interpretationBeyond picomolar affinities: quantitative aspects of noncovalent and covalent binding of drugs to proteinsNew agents for the treatment of drug-resistant Mycobacterium tuberculosisPTH receptor-1 signalling-mechanistic insights and therapeutic prospectsApplications of SPR for the characterization of molecules important in the pathogenesis and treatment of neurodegenerative diseasesTrapping conformational states along ligand-binding dynamics of peptide deformylase: the impact of induced fit on enzyme catalysis1a/1b Subtype Profiling of Nonnucleoside Polymerase Inhibitors of Hepatitis C VirusAn Arginine Switch in the Species B Adenovirus Knob Determines High-Affinity Engagement of Cellular Receptor CD46Slow-Onset Inhibition of the FabI Enoyl Reductase from Francisella tularensis : Residence Time and in Vivo ActivityA Slow, Tight Binding Inhibitor of InhA, the Enoyl-Acyl Carrier Protein Reductase from Mycobacterium tuberculosisMalarial dihydrofolate reductase as a paradigm for drug development against a resistance-compromised targetStructure-kinetic relationship study of CDK8/CycC specific compoundsRational Optimization of Drug-Target Residence Time: Insights from Inhibitor Binding to the Staphylococcus aureus FabI Enzyme–Product ComplexReversible targeting of noncatalytic cysteines with chemically tuned electrophilesStructure-based macrocyclization yields hepatitis C virus NS5B inhibitors with improved binding affinities and pharmacokinetic propertiesPotent inhibition of DOT1L as treatment of MLL-fusion leukemiaHistone Deacetylase (HDAC) Inhibitor Kinetic Rate Constants Correlate with Cellular Histone Acetylation but Not Transcription and Cell ViabilityStructural Basis for the Recognition of Mycolic Acid Precursors by KasA, a Condensing Enzyme and Drug Target from Mycobacterium TuberculosisA structural and energetic model for the slow-onset inhibition of the Mycobacterium tuberculosis enoyl-ACP reductase InhA.Time-Dependent Diaryl Ether Inhibitors of InhA: Structure-Activity Relationship Studies of Enzyme Inhibition, Antibacterial Activity, and in vivo EfficacyConformational adaptation drives potent, selective and durable inhibition of the human protein methyltransferase DOT1LOptimized inhibitors of soluble epoxide hydrolase improve in vitro target residence time and in vivo efficacyInsight into the Inhibition of Drug-Resistant Mutants of the Receptor Tyrosine Kinase EGFRDrug discovery using chemical systems biology: weak inhibition of multiple kinases may contribute to the anti-cancer effect of nelfinavirVirtual screening, identification and in vitro testing of novel inhibitors of O-acetyl-L-serine sulfhydrylase of Entamoeba histolyticaTowards structural systems pharmacology to study complex diseases and personalized medicineEnsemble generation and the influence of protein flexibility on geometric tunnel prediction in cytochrome P450 enzymesP-loop conformation governed crizotinib resistance in G2032R-mutated ROS1 tyrosine kinase: clues from free energy landscapeThe universal statistical distributions of the affinity, equilibrium constants, kinetics and specificity in biomolecular recognitionSlow-Onset Inhibition of Mycobacterium tuberculosis InhA: Revealing Molecular Determinants of Residence Time by MD SimulationsTranslational Nano-Medicines: Targeted Therapeutic Delivery for Cancer and Inflammatory DiseasesA Four-Point Screening Method for Assessing Molecular Mechanism of Action (MMOA) Identifies Tideglusib as a Time-Dependent Inhibitor of Trypanosoma brucei GSK3βComparing the epidermal growth factor interaction with four different cell lines: intriguing effects imply strong dependency of cellular contextCinnamide Derivatives of d-Mannose as Inhibitors of the Bacterial Virulence Factor LecB from Pseudomonas aeruginosaLight-controlled modulation of gene expression by chemical optoepigenetic probesOpicapone: a short lived and very long acting novel catechol-O-methyltransferase inhibitor following multiple dose administration in healthy subjectsTargeting Non-Catalytic Cysteine Residues Through Structure-Guided Drug Discovery
P2860
Q24322769-2418D4D2-5E83-4848-8FF5-7EA1996CEC1BQ24595639-177BADD0-D6CF-4854-A767-39246FFA7B6BQ24600175-A37A373E-588C-43EF-BEAD-ACD0CF51E5FFQ24629851-4B0EFDA9-AF76-4217-9388-12257CFBBAD2Q24649147-60428B74-0E52-413F-9A89-77CA83952E10Q26751463-5D27B2ED-871A-4EDE-AB6F-23FE3D41C191Q26798005-61547FED-57C9-47A6-AF37-51ED27AAD561Q26860077-9495B107-D641-4EF7-964E-303905F0BCA5Q27321405-D9E1AEE2-B88A-4279-9C75-E9D8962DAE68Q27490956-2D4DB1BF-8CEB-4FC4-82AF-DDD03BDAE885Q27652785-4E583F3B-BDAE-44BE-A802-F29A959E7F6BQ27653711-2623F6F0-A7F9-41D6-9867-949F92AE8F21Q27660104-6E682171-530A-4EB1-9D87-42DB4D6DFF10Q27674154-161AB1BE-6744-49EE-AD13-40358B460686Q27677859-3427C4B2-C14E-4E2D-9C8D-C2FE36EA3259Q27678258-84501D38-C60E-4CBC-B101-250A69EB6B3CQ27678280-ED1C0132-2DB7-41A1-AABF-C339D0AA68C9Q27678311-4E664AEC-CD14-427C-A042-846764BBE929Q27678800-FB5FA2CB-1274-4291-87F2-BAA222296529Q27679266-DB021136-ACB0-459B-B051-0F8073C1E051Q27680210-A4A7B7B8-95A0-4F6C-ABDD-3F9515C4689DQ27681724-936867DE-474D-48DF-AE30-375BE40D3D62Q27682088-44A7B261-A69B-4A93-9D35-EAB424B9ED3EQ27682251-1BC7BB69-DD6C-4E86-94DC-4A6AD30C404BQ27684895-1421920D-26F8-49D6-A592-557BC77307EBQ27725743-83EC10AF-CFE1-4403-875F-D3FB5007F1D7Q28477930-7EA059EE-816B-4615-AD8F-F25C3C44F472Q28480744-098D7F4A-C9CA-425C-A5B4-1902A81E00D8Q28538838-93743A66-D8B8-402F-9C52-ED6046A92407Q28539919-BDFD86B0-3731-44AA-997D-D17FF239D728Q28540825-23B0C4BA-0C97-4668-8132-DC16B182F96FQ28546498-408E302A-ADDE-422F-9682-362DC7BB44D3Q28547385-62269C20-666B-463F-8ED1-19414963F117Q28548580-E76202BA-2615-4129-A100-3731E5858C05Q28550557-F7684EE7-30A3-428A-92BF-CA73C23521FAQ28743143-FA8C38BA-B448-42D2-8BA5-952C4B333D8BQ28830444-86594F24-7D53-48B7-BD2B-A37BA8049B9BQ28834530-24FA9A4B-99A6-4DFE-8CFB-BD08C12E855EQ29391915-5B7D3F43-F515-4823-B7D3-27840C8608BBQ30390894-CB621819-6474-4757-81F2-AA7318003445
P2860
Drug-target residence time and its implications for lead optimization.
description
2006 nî lūn-bûn
@nan
2006年の論文
@ja
2006年論文
@yue
2006年論文
@zh-hant
2006年論文
@zh-hk
2006年論文
@zh-mo
2006年論文
@zh-tw
2006年论文
@wuu
2006年论文
@zh
2006年论文
@zh-cn
name
Drug-target residence time and its implications for lead optimization.
@ast
Drug-target residence time and its implications for lead optimization.
@en
type
label
Drug-target residence time and its implications for lead optimization.
@ast
Drug-target residence time and its implications for lead optimization.
@en
prefLabel
Drug-target residence time and its implications for lead optimization.
@ast
Drug-target residence time and its implications for lead optimization.
@en
P2093
P356
P1476
Drug-target residence time and its implications for lead optimization.
@en
P2093
David L Pompliano
Robert A Copeland
Thomas D Meek
P2888
P304
P356
10.1038/NRD2082
P577
2006-08-04T00:00:00Z