Discovery of a small-molecule HIV-1 integrase inhibitor-binding site
about
Crystal structure of the HIV-1 integrase core domain in complex with sucrose reveals details of an allosteric inhibitory binding siteMultimode, Cooperative Mechanism of Action of Allosteric HIV-1 Integrase InhibitorsNew Class of HIV-1 Integrase (IN) Inhibitors with a Dual Mode of ActionA historical sketch of the discovery and development of HIV-1 integrase inhibitorsA symmetric region of the HIV-1 integrase dimerization interface is essential for viral replicationNon-catalytic site HIV-1 integrase inhibitors disrupt core maturation and induce a reverse transcription block in target cellsPhotoaffinity labeling combined with mass spectrometric approaches as a tool for structural proteomics.An allosteric mechanism for inhibiting HIV-1 integrase with a small molecule.HIV-1 IN inhibitors: 2010 update and perspectivesPeptides that inhibit HIV-1 integrase by blocking its protein-protein interactions.Allosteric inhibitor development targeting HIV-1 integrase.FRET analysis reveals distinct conformations of IN tetramers in the presence of viral DNA or LEDGF/p75.Clinical Use of Inhibitors of HIV-1 Integration: Problems and Prospects.Hybrid quantum mechanical/molecular mechanical molecular dynamics simulations of HIV-1 integrase/inhibitor complexes.Dynamic modulation of HIV-1 integrase structure and function by cellular lens epithelium-derived growth factor (LEDGF) protein.Integrase, LEDGF/p75 and HIV replication.In search of small molecules blocking interactions between HIV proteins and intracellular cofactors.Binding ensemble profiling with photoaffinity labeling (BEProFL) approach: mapping the binding poses of HDAC8 inhibitorsMultimodal mechanism of action of allosteric HIV-1 integrase inhibitors.Inhibitors of the interactions between HIV-1 IN and the cofactor LEDGF/p75.Mass spectrometry-based structural proteomics."Old Dogs with New Tricks": exploiting alternative mechanisms of action and new drug design strategies for clinically validated HIV targets.HIV-1 integrase multimerization as a therapeutic target.3-Phenylcoumarins as inhibitors of HIV-1 replication.Inhibition of dengue virus polymerase by blocking of the RNA tunnelInhibiting the HIV integration process: past, present, and the future.Target Identification by Diazirine Photo-Cross-linking and Click Chemistry.Covalent Inhibition of HIV-1 Integrase by N-Succinimidyl Peptides.Examining the mechanism of action of a kinesin inhibitor using stable isotope labeled inhibitors for cross-linking (SILIC).Discovery of small-molecule HIV-1 fusion and integrase inhibitors oleuropein and hydroxytyrosol: part II. integrase inhibition.Computer-aided design and discovery of protein-protein interaction inhibitors as agents for anti-HIV therapy.Probing the conformation of the ISWI ATPase domain with genetically encoded photoreactive crosslinkers and mass spectrometry.Defining the DNA substrate binding sites on HIV-1 integrase.Concise synthesis and anti-HIV activity of pyrimido[1,2-c][1,3]benzothiazin-6-imines and related tricyclic heterocycles.Inhibitory profile of a LEDGF/p75 peptide against HIV-1 integrase: insight into integrase-DNA complex formation and catalysis.Development of an AlphaScreen-based HIV-1 integrase dimerization assay for discovery of novel allosteric inhibitors.Insight into the inhibitory mechanism and binding mode between D77 and HIV-1 integrase by molecular modeling methods.Single amino acid substitution in HIV-1 integrase catalytic core causes a dramatic shift in inhibitor selectivity.
P2860
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P2860
Discovery of a small-molecule HIV-1 integrase inhibitor-binding site
description
2006 nî lūn-bûn
@nan
2006 թուականի Յունիսին հրատարակուած գիտական յօդուած
@hyw
2006 թվականի հունիսին հրատարակված գիտական հոդված
@hy
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
name
Discovery of a small-molecule HIV-1 integrase inhibitor-binding site
@ast
Discovery of a small-molecule HIV-1 integrase inhibitor-binding site
@en
Discovery of a small-molecule HIV-1 integrase inhibitor-binding site
@nl
type
label
Discovery of a small-molecule HIV-1 integrase inhibitor-binding site
@ast
Discovery of a small-molecule HIV-1 integrase inhibitor-binding site
@en
Discovery of a small-molecule HIV-1 integrase inhibitor-binding site
@nl
prefLabel
Discovery of a small-molecule HIV-1 integrase inhibitor-binding site
@ast
Discovery of a small-molecule HIV-1 integrase inhibitor-binding site
@en
Discovery of a small-molecule HIV-1 integrase inhibitor-binding site
@nl
P2093
P2860
P356
P1476
Discovery of a small-molecule HIV-1 integrase inhibitor-binding site
@en
P2093
Christoph H Borchers
Laith Q Al-Mawsawi
Myriam Witvrouw
Nouri Neamati
Raveendra Dayam
Terrence R Burke
Valery Fikkert
P2860
P304
10080-10085
P356
10.1073/PNAS.0511254103
P407
P577
2006-06-19T00:00:00Z