Zeger Debyser

Characterization of lentiviral vector-mediated gene transfer in adult mouse brain.

DNA-induced polymerization of HIV-1 integrase analyzed with fluorescence fluctuation spectroscopy.

New class of HIV integrase inhibitors that block viral replication in cell culture.

In search of authentic inhibitors of HIV-1 integration.

Inhibition of human immunodeficiency virus type 1 integration by diketo derivatives.

HIV-1 integrase forms stable tetramers and associates with LEDGF/p75 protein in human cells.

env chimeric virus technology for evaluating human immunodeficiency virus susceptibility to entry inhibitors.

Establishment of an in vitro assay system mimicking human immunodeficiency virus type 1-induced neural cell death and evaluation of inhibitors thereof.

Impact of the central polypurine tract on the kinetics of human immunodeficiency virus type 1 vector transduction.

N-aminoimidazole derivatives inhibiting retroviral replication via a yet unidentified mode of action.

LEDGF/p75 is essential for nuclear and chromosomal targeting of HIV-1 integrase in human cells.

Neuropathology and neurodegeneration in rodent brain induced by lentiviral vector-mediated overexpression of alpha-synuclein.

Development of resistance against diketo derivatives of human immunodeficiency virus type 1 by progressive accumulation of integrase mutations.

Lentiviral vector-mediated delivery of short hairpin RNA results in persistent knockdown of gene expression in mouse brain.

A short course on virology / vectorology / gene therapy.

Biosafety of lentiviral vectors.

Expression of HIV-1 integrase in CEM cells inhibits HIV-1 replication.

Identification and characterization of a functional nuclear localization signal in the HIV-1 integrase interactor LEDGF/p75.

Efficient 3D database screening for novel HIV-1 IN inhibitors.

Multiple mutations in human immunodeficiency virus-1 integrase confer resistance to the clinical trial drug S-1360.

Evaluation of the activity of HIV-1 integrase over-expressed in eukaryotic cells.

Positional effects of the central DNA flap in HIV-1-derived lentiviral vectors.

The interaction of LEDGF/p75 with integrase is lentivirus-specific and promotes DNA binding.

Measuring protein-protein interactions inside living cells using single color fluorescence correlation spectroscopy. Application to human immunodeficiency virus type 1 integrase and LEDGF/p75.

Integrase mutants defective for interaction with LEDGF/p75 are impaired in chromosome tethering and HIV-1 replication.

HIV-1 integration: an interplay between HIV-1 integrase, cellular and viral proteins.

Hematopoietic stem cell-based gene therapy against HIV infection: promises and caveats.

Upscaling of lentiviral vector production by tangential flow filtration.

Mutations in both env and gag genes are required for HIV-1 resistance to the polysulfonic dendrimer SPL2923, as corroborated by chimeric virus technology.

Pharmacophore-based design of HIV-1 integrase strand-transfer inhibitors.

Cellular co-factors of HIV-1 integration.

The aggregation of alpha-synuclein is stimulated by FK506 binding proteins as shown by fluorescence correlation spectroscopy.

Non-invasive imaging of neuropathology in a rat model of alpha-synuclein overexpression.

Transient and stable knockdown of the integrase cofactor LEDGF/p75 reveals its role in the replication cycle of human immunodeficiency virus.

Lentiviral vectors mediate efficient and stable gene transfer in adult neural stem cells in vivo.

Noninvasive monitoring of long-term lentiviral vector-mediated gene expression in rodent brain with bioluminescence imaging.

Comparison of lentiviral vector titration methods.

Parkin protects against neurotoxicity in the 6-hydroxydopamine rat model for Parkinson's disease.

The central DNA flap of the human immunodeficiency virus type 1 is important for viral replication.

Overexpression of the lens epithelium-derived growth factor/p75 integrase binding domain inhibits human immunodeficiency virus replication.

Concise review: therapeutic strategies for Parkinson disease based on the modulation of adult neurogenesis.

Identification of the LEDGF/p75 binding site in HIV-1 integrase.

Simple criterion for selection of flavonoid compounds with anti-HIV activity.

Synthesis and preliminary evaluation of 18F- or 11C-labeled bicyclic nucleoside analogues as potential probes for imaging varicella-zoster virus thymidine kinase gene expression using positron emission tomography.

Comparative analysis of adeno-associated viral vector serotypes 1, 2, 5, 7, and 8 in mouse brain.

Virus evolution reveals an exclusive role for LEDGF/p75 in chromosomal tethering of HIV.

Fetal gene transfer with lentiviral vectors: long-term in vivo follow-up evaluation in a rat model.

Synthesis and biological evaluation of an 123I-labeled bicyclic nucleoside analogue (BCNA) as potential SPECT tracer for VZV-tk reporter gene imaging.

Lentiviral nuclear import: a complex interplay between virus and host.

New 4-[(1-benzyl-1H-indol-3-yl)carbonyl]-3-hydroxyfuran-2(5H)-ones, beta-diketo acid analogs as HIV-1 integrase inhibitors.

Novel virtual screening protocol based on the combined use of molecular modeling and electron-ion interaction potential techniques to design HIV-1 integrase inhibitors.

Differential interaction of HIV-1 integrase and JPO2 with the C terminus of LEDGF/p75.

Toward novel HIV-1 integrase binding inhibitors: molecular modeling, synthesis, and biological studies.

Local origin and activity-dependent generation of nestin-expressing protoplasmic astrocytes in CA1.

Discovery of novel non-cytotoxic salicylhydrazide containing HIV-1 integrase inhibitors.

Efficient purification and metabolite analysis of radiotracers using high-performance liquid chromatography and on-line solid-phase extraction.

A p-[18F]fluoroethoxyphenyl bicyclic nucleoside analogue as a potential positron emission tomography imaging agent for varicella-zoster virus thymidine kinase gene expression.

Synthesis and evaluation of 18F- and 11C-labeled phenyl-galactopyranosides as potential probes for in vivo visualization of LacZ gene expression using positron emission tomography.

Diffusion of myelin oligodendrocyte glycoprotein in living OLN-93 cells investigated by raster-scanning image correlation spectroscopy (RICS).

The total synthesis of fukiic acid, an HIV-1 integrase inhibitor.

Quinolone 3-carboxylic acid pharmacophore: design of second generation HIV-1 integrase inhibitors.

Inhibitory profile of a LEDGF/p75 peptide against HIV-1 integrase: insight into integrase-DNA complex formation and catalysis.

FK506 binding protein 12 differentially accelerates fibril formation of wild type alpha-synuclein and its clinical mutants A30P or A53T.

Reaction of rosmarinic acid with nitrite ions in acidic conditions: discovery of nitro- and dinitrorosmarinic acids as new anti-HIV-1 agents.

Mutations in human immunodeficiency virus type 1 integrase confer resistance to the naphthyridine L-870,810 and cross-resistance to the clinical trial drug GS-9137.

A refined pharmacophore model for HIV-1 integrase inhibitors: Optimization of potency in the 1H-benzylindole series.

Four-tiered pi interaction at the dimeric interface of HIV-1 integrase critical for DNA integration and viral infectivity.

Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors.

Noninvasive and quantitative monitoring of adult neuronal stem cell migration in mouse brain using bioluminescence imaging.

Investigations on the 4-quinolone-3-carboxylic acid motif. 1. Synthesis and structure-activity relationship of a class of human immunodeficiency virus type 1 integrase inhibitors.

Synthesis and antiviral properties of some polyphenols related to Salvia genus.

Alternative splicing and caspase-mediated cleavage generate antagonistic variants of the stress oncoprotein LEDGF/p75.

Transportin-SR2 imports HIV into the nucleus.

Novel targets for HIV therapy.

Design, synthesis, and biological evaluation of a series of 2-hydroxyisoquinoline-1,3(2H,4H)-diones as dual inhibitors of human immunodeficiency virus type 1 integrase and the reverse transcriptase RNase H domain.

In search of small molecules blocking interactions between HIV proteins and intracellular cofactors.

Docking studies on a new human immunodeficiency virus integrase-Mg-DNA complex: phenyl ring exploration and synthesis of 1H-benzylindole derivatives through fluorine substitutions.

Lens epithelium-derived growth factor/p75 interacts with the transposase-derived DDE domain of PogZ.

Targeting the HIV integration process in antiviral therapy.

Highly efficient multicistronic lentiviral vectors with peptide 2A sequences.

Exploration of novel thiobarbituric acid-, rhodanine- and thiohydantoin-based HIV-1 integrase inhibitors.

Synthesis and biological evaluation of (11)C-labeled beta-galactosyl triazoles as potential PET tracers for in vivo LacZ reporter gene imaging.

Seeing genes at work in the living brain with non-invasive molecular imaging.

Pharmacophore-based discovery of small-molecule inhibitors of protein-protein interactions between HIV-1 integrase and cellular cofactor LEDGF/p75.

Fetal surgery is a clinical reality.

State-of-the-art lentiviral vectors for research use: risk assessment and biosafety recommendations.

Inhibition of FK506 binding proteins reduces alpha-synuclein aggregation and Parkinson's disease-like pathology.

Immunohistochemical detection of transgene expression in the brain using small epitope tags.

Morphologic and functional changes in the unilateral 6-hydroxydopamine lesion rat model for Parkinson's disease discerned with microSPECT and quantitative MRI.

LEDGF hybrids efficiently retarget lentiviral integration into heterochromatin.

Differential effects of progenitor cell populations on left ventricular remodeling and myocardial neovascularization after myocardial infarction.

Rational design of small-molecule inhibitors of the LEDGF/p75-integrase interaction and HIV replication.

High-resolution profiling of the LEDGF/p75 chromatin interaction in the ENCODE region.

Rapid, simple, and versatile manufacturing of recombinant adeno-associated viral vectors at scale.

New 2-arylnaphthalenediols and triol inhibitors of HIV-1 integrase--discovery of a new polyhydroxylated antiviral agent.

New chloro,fluorobenzylindole derivatives as integrase strand-transfer inhibitors (INSTIs) and their mode of action.

Efficient gene transfer into the mouse lung by fetal intratracheal injection of rAAV2/6.2.

Small molecules targeting the interaction between HIV-1 integrase and LEDGF/p75 cofactor.

The transcriptional co-activator LEDGF/p75 displays a dynamic scan-and-lock mechanism for chromatin tethering.

2-hydroxyisoquinoline-1,3(2H,4H)-diones as inhibitors of HIV-1 integrase and reverse transcriptase RNase H domain: influence of the alkylation of position 4.

HIV-1 integrase strand-transfer inhibitors: design, synthesis and molecular modeling investigation.

A versatile and practical synthesis toward the development of novel HIV-1 integrase inhibitors.

Interplay between HIV entry and transportin-SR2 dependency.

Magnesium chelating 2-hydroxyisoquinoline-1,3(2H,4H)-diones, as inhibitors of HIV-1 integrase and/or the HIV-1 reverse transcriptase ribonuclease H domain: discovery of a novel selective inhibitor of the ribonuclease H function.

Depletion of PINK1 affects mitochondrial metabolism, calcium homeostasis and energy maintenance.

In search of second-generation HIV integrase inhibitors: targeting integration beyond strand transfer.

Unraveling the role of peptidyl-prolyl isomerases in neurodegeneration.

Comparative analysis of different peptidyl-prolyl isomerases reveals FK506-binding protein 12 as the most potent enhancer of alpha-synuclein aggregation.

A PET brain reporter gene system based on type 2 cannabinoid receptors.

Association of polymorphisms in the LEDGF/p75 gene (PSIP1) with susceptibility to HIV-1 infection and disease progression.

Toward the discovery of novel anti-HIV drugs. Second-generation inhibitors of the cellular ATPase DDX3 with improved anti-HIV activity: synthesis, structure-activity relationship analysis, cytotoxicity studies, and target validation.

miR669a and miR669q prevent skeletal muscle differentiation in postnatal cardiac progenitors.

Synthesis, in vitro and in vivo evaluation of fluorine-18 labelled FE-GW405833 as a PET tracer for type 2 cannabinoid receptor imaging.

In vitro DNA tethering of HIV-1 integrase by the transcriptional coactivator LEDGF/p75.

Rilpivirine: a step forward in tailored HIV treatment.

4-[1-(4-Fluorobenzyl)-4-hydroxy-1H-indol-3-yl]-2-hydroxy-4-oxobut-2-enoic acid as a prototype to develop dual inhibitors of HIV-1 integration process.

Pathway specific gene expression profiling reveals oxidative stress genes potentially regulated by transcription co-activator LEDGF/p75 in prostate cancer cells.

Role of the PWWP domain of lens epithelium-derived growth factor (LEDGF)/p75 cofactor in lentiviral integration targeting.

Elvitegravir: a once daily alternative to raltegravir.

Preclinical evaluation of [11C]NE40, a type 2 cannabinoid receptor PET tracer.

Nitrogen-containing polyhydroxylated aromatics as HIV-1 integrase inhibitors: synthesis, structure-activity relationship analysis, and biological activity.

The stress oncoprotein LEDGF/p75 interacts with the methyl CpG binding protein MeCP2 and influences its transcriptional activity.

Regulator of G-protein signaling 18 controls megakaryopoiesis and the cilia-mediated vertebrate mechanosensory system.

Lens epithelium-derived growth factor/p75 qualifies as a target for HIV gene therapy in the NSG mouse model.

Development of an AlphaScreen-based HIV-1 integrase dimerization assay for discovery of novel allosteric inhibitors.

LEDGF/p75-independent HIV-1 replication demonstrates a role for HRP-2 and remains sensitive to inhibition by LEDGINs.

Discovery of small molecule HIV-1 integrase dimerization inhibitors.

Development of a series of 3-hydroxyquinolin-2(1H)-ones as selective inhibitors of HIV-1 reverse transcriptase associated RNase H activity.

Galectin-1 in melanoma biology and related neo-angiogenesis processes.

Small-molecule inhibitors of the LEDGF/p75 binding site of integrase block HIV replication and modulate integrase multimerization.

Quantitative evaluation of MRI-based tracking of ferritin-labeled endogenous neural stem cell progeny in rodent brain.

Quad's in it for antiretroviral therapy?

Fragment hopping approach directed at design of HIV IN-LEDGF/p75 interaction inhibitors.

Phage Display-directed Discovery of LEDGF/p75 Binding Cyclic Peptide Inhibitors of HIV Replication.

Combinational therapies for HIV: a focus on EVG/COBI/FTC/TDF.

Identification of Residues in the C-terminal Domain of HIV-1 Integrase That Mediate Binding to the Transportin-SR2 Protein.

Interaction of the HIV-1 Intasome with Transportin 3 Protein (TNPO3 or TRN-SR2).

Cellular cofactors of lentiviral integrase: from target validation to drug discovery.

Preliminary validation of varicella zoster virus thymidine kinase as a novel reporter gene for PET.

A Symmetric Region of the HIV-1 Integrase Dimerization Interface Is Essential for Viral Replication.

HRP-2 determines HIV-1 integration site selection in LEDGF/p75 depleted cells.