Published in ChemMedChem on August 01, 2009
Rational design of small-molecule inhibitors of the LEDGF/p75-integrase interaction and HIV replication. Nat Chem Biol (2010) 2.48
HIV-1 IN inhibitors: 2010 update and perspectives. Curr Top Med Chem (2009) 1.53
New class of HIV-1 integrase (IN) inhibitors with a dual mode of action. J Biol Chem (2012) 1.52
Non-catalytic site HIV-1 integrase inhibitors disrupt core maturation and induce a reverse transcription block in target cells. PLoS One (2013) 1.29
Allosteric inhibitor development targeting HIV-1 integrase. ChemMedChem (2011) 1.00
Preclinical profile of BI 224436, a novel HIV-1 non-catalytic-site integrase inhibitor. Antimicrob Agents Chemother (2014) 0.96
Inhibiting the HIV integration process: past, present, and the future. J Med Chem (2013) 0.93
Multimodal mechanism of action of allosteric HIV-1 integrase inhibitors. Expert Rev Mol Med (2013) 0.92
Hit identification and optimization in virtual screening: practical recommendations based on a critical literature analysis. J Med Chem (2013) 0.86
Design of HIV-1 integrase inhibitors targeting the catalytic domain as well as its interaction with LEDGF/p75: a scaffold hopping approach using salicylate and catechol groups. Bioorg Med Chem (2011) 0.85
From laptop to benchtop to bedside: structure-based drug design on protein targets. Curr Pharm Des (2012) 0.85
Interrogating HIV integrase for compounds that bind--a SAMPL challenge. J Comput Aided Mol Des (2014) 0.85
The Interaction Between Lentiviral Integrase and LEDGF: Structural and Functional Insights. Viruses (2009) 0.85
Cellular cofactors of lentiviral integrase: from target validation to drug discovery. Mol Biol Int (2012) 0.81
Three-dimensional compound comparison methods and their application in drug discovery. Molecules (2015) 0.81
Evidence of conformational selection driving the formation of ligand binding sites in protein-protein interfaces. PLoS Comput Biol (2014) 0.81
A symmetric region of the HIV-1 integrase dimerization interface is essential for viral replication. PLoS One (2012) 0.79
Identification of old drugs as potential inhibitors of HIV-1 integrase - human LEDGF/p75 interaction via molecular docking. J Mol Model (2012) 0.79
Clinical Use of Inhibitors of HIV-1 Integration: Problems and Prospects. Acta Naturae (2011) 0.78
Prospective strategies for targeting HIV-1 integrase function. Future Med Chem (2010) 0.78
Different Pathways Leading to Integrase Inhibitors Resistance. Front Microbiol (2017) 0.77
A New Class of Allosteric HIV-1 Integrase Inhibitors Identified by Crystallographic Fragment Screening of the Catalytic Core Domain. J Biol Chem (2016) 0.75
Ultra-High-Throughput Structure-Based Virtual Screening for Small-Molecule Inhibitors of Protein-Protein Interactions. J Chem Inf Model (2016) 0.75
HIV-1 integrase forms stable tetramers and associates with LEDGF/p75 protein in human cells. J Biol Chem (2002) 4.91
LEDGF/p75 is essential for nuclear and chromosomal targeting of HIV-1 integrase in human cells. J Biol Chem (2003) 3.97
Comparative analysis of adeno-associated viral vector serotypes 1, 2, 5, 7, and 8 in mouse brain. Hum Gene Ther (2007) 2.64
Rapid, simple, and versatile manufacturing of recombinant adeno-associated viral vectors at scale. Hum Gene Ther (2010) 2.51
Rational design of small-molecule inhibitors of the LEDGF/p75-integrase interaction and HIV replication. Nat Chem Biol (2010) 2.48
Integrase mutants defective for interaction with LEDGF/p75 are impaired in chromosome tethering and HIV-1 replication. J Biol Chem (2005) 2.44
Transportin-SR2 imports HIV into the nucleus. Curr Biol (2008) 2.35
The interaction of LEDGF/p75 with integrase is lentivirus-specific and promotes DNA binding. J Biol Chem (2005) 2.28
Photodynamic therapy in the treatment of microbial infections: basic principles and perspective applications. Lasers Surg Med (2006) 2.27
Transient and stable knockdown of the integrase cofactor LEDGF/p75 reveals its role in the replication cycle of human immunodeficiency virus. J Virol (2006) 2.09
Synthesis and anti-hIV activity of 1-(2,6-difluorophenyl)-1H,3H-thiazolo[3,4-a]benzimidazole structurally-related 1,2-substituted benzimidazoles. Farmaco (2002) 2.04
Long-term reversal of diabetes in non-obese diabetic mice by liver-directed gene therapy. J Gene Med (2013) 2.02
Overexpression of the lens epithelium-derived growth factor/p75 integrase binding domain inhibits human immunodeficiency virus replication. J Virol (2006) 1.82
LEDGF hybrids efficiently retarget lentiviral integration into heterochromatin. Mol Ther (2010) 1.72
Differential effects of progenitor cell populations on left ventricular remodeling and myocardial neovascularization after myocardial infarction. J Am Coll Cardiol (2010) 1.70
Cellular co-factors of HIV-1 integration. Trends Biochem Sci (2006) 1.68
Impact of the central polypurine tract on the kinetics of human immunodeficiency virus type 1 vector transduction. J Virol (2003) 1.61
Highly efficient multicistronic lentiviral vectors with peptide 2A sequences. Hum Gene Ther (2009) 1.54
Development of resistance against diketo derivatives of human immunodeficiency virus type 1 by progressive accumulation of integrase mutations. J Virol (2003) 1.54
Design, synthesis, structure-activity relationships, and molecular modeling studies of 2,3-diaryl-1,3-thiazolidin-4-ones as potent anti-HIV agents. J Med Chem (2002) 1.51
Characterization of lentiviral vector-mediated gene transfer in adult mouse brain. Hum Gene Ther (2002) 1.50
Identification and characterization of a functional nuclear localization signal in the HIV-1 integrase interactor LEDGF/p75. J Biol Chem (2004) 1.47
Comparison of lentiviral vector titration methods. BMC Biotechnol (2006) 1.42
Virus evolution reveals an exclusive role for LEDGF/p75 in chromosomal tethering of HIV. PLoS Pathog (2007) 1.41
Small-molecule inhibitors of the LEDGF/p75 binding site of integrase block HIV replication and modulate integrase multimerization. Antimicrob Agents Chemother (2012) 1.40
Upscaling of lentiviral vector production by tangential flow filtration. J Gene Med (2005) 1.38
Lens epithelium-derived growth factor/p75 interacts with the transposase-derived DDE domain of PogZ. J Biol Chem (2009) 1.30
5-Arylidene-2-imino-4-thiazolidinones: design and synthesis of novel anti-inflammatory agents. Bioorg Med Chem (2005) 1.29
Multiple mutations in human immunodeficiency virus-1 integrase confer resistance to the clinical trial drug S-1360. AIDS (2004) 1.28
p53 is a direct transcriptional target of MYCN in neuroblastoma. Cancer Res (2010) 1.27
The BET family of proteins targets moloney murine leukemia virus integration near transcription start sites. Cell Rep (2013) 1.26
Activation of tissue transglutaminase transcription by histone deacetylase inhibition as a therapeutic approach for Myc oncogenesis. Proc Natl Acad Sci U S A (2007) 1.26
A highly intensified ART regimen induces long-term viral suppression and restriction of the viral reservoir in a simian AIDS model. PLoS Pathog (2012) 1.26
LEDGF/p75-independent HIV-1 replication demonstrates a role for HRP-2 and remains sensitive to inhibition by LEDGINs. PLoS Pathog (2012) 1.25
Identification of the LEDGF/p75 binding site in HIV-1 integrase. J Mol Biol (2006) 1.24
Lentiviral nuclear import: a complex interplay between virus and host. Bioessays (2007) 1.22
The stem cell secretome and its role in brain repair. Biochimie (2013) 1.19
LEDGINs inhibit late stage HIV-1 replication by modulating integrase multimerization in the virions. Retrovirology (2013) 1.17
Interplay between HIV entry and transportin-SR2 dependency. Retrovirology (2011) 1.17
Discovery of novel non-cytotoxic salicylhydrazide containing HIV-1 integrase inhibitors. Bioorg Med Chem Lett (2007) 1.16
Fetal surgery is a clinical reality. Semin Fetal Neonatal Med (2009) 1.15
Discovery of novel benzimidazolones as potent non-nucleoside reverse transcriptase inhibitors active against wild-type and mutant HIV-1 strains. Bioorg Med Chem Lett (2007) 1.15
Novel targets for HIV therapy. Antiviral Res (2008) 1.15
IKAROS deletions dictate a unique gene expression signature in patients with adult B-cell acute lymphoblastic leukemia. PLoS One (2012) 1.15
Differential interaction of HIV-1 integrase and JPO2 with the C terminus of LEDGF/p75. J Mol Biol (2007) 1.14
Response of a simian immunodeficiency virus (SIVmac251) to raltegravir: a basis for a new treatment for simian AIDS and an animal model for studying lentiviral persistence during antiretroviral therapy. Retrovirology (2010) 1.13
New class of HIV integrase inhibitors that block viral replication in cell culture. Curr Biol (2002) 1.13
Noninvasive monitoring of long-term lentiviral vector-mediated gene expression in rodent brain with bioluminescence imaging. Mol Ther (2006) 1.11
Lentiviral vector-mediated delivery of short hairpin RNA results in persistent knockdown of gene expression in mouse brain. Hum Gene Ther (2003) 1.11
Depletion of PINK1 affects mitochondrial metabolism, calcium homeostasis and energy maintenance. J Cell Sci (2011) 1.11
ABCC multidrug transporters in childhood neuroblastoma: clinical and biological effects independent of cytotoxic drug efflux. J Natl Cancer Inst (2011) 1.11
Design of a novel cyclotide-based CXCR4 antagonist with anti-human immunodeficiency virus (HIV)-1 activity. J Med Chem (2012) 1.10
Synthesis and antibacterial activity of new poly-S-lysine-porphyrin conjugates. J Med Chem (2004) 1.10
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. Antimicrob Agents Chemother (2008) 1.10
Quantitative evaluation of MRI-based tracking of ferritin-labeled endogenous neural stem cell progeny in rodent brain. Neuroimage (2012) 1.10
The LEDGF/p75 integrase interaction, a novel target for anti-HIV therapy. Virology (2013) 1.10
Novel N1-substituted 1,3-dihydro-2H-benzimidazol-2-ones as potent non-nucleoside reverse transcriptase inhibitors. Bioorg Med Chem (2008) 1.09
High-resolution profiling of the LEDGF/p75 chromatin interaction in the ENCODE region. Nucleic Acids Res (2010) 1.08
The transcriptional co-activator LEDGF/p75 displays a dynamic scan-and-lock mechanism for chromatin tethering. Nucleic Acids Res (2010) 1.08
Novel potent anticonvulsant agent containing a tetrahydroisoquinoline skeleton. J Med Chem (2006) 1.06
Anti-HIV agents: design and discovery of new potent RT inhibitors. Farmaco (2003) 1.06
HIV-1 integration: an interplay between HIV-1 integrase, cellular and viral proteins. AIDS Rev (2005) 1.04
Alternative splicing and caspase-mediated cleavage generate antagonistic variants of the stress oncoprotein LEDGF/p75. Mol Cancer Res (2008) 1.04
Pharmacophore-based design of HIV-1 integrase strand-transfer inhibitors. J Med Chem (2005) 1.04
env chimeric virus technology for evaluating human immunodeficiency virus susceptibility to entry inhibitors. Antimicrob Agents Chemother (2002) 1.04
Synthesis and anti-HIV activity of 2,3-diaryl-1,3-thiazolidin-4-ones. Farmaco (2003) 1.03
Molecular dynamics studies of the full-length integrase-DNA complex. Biochem Biophys Res Commun (2005) 1.03
Role of the PWWP domain of lens epithelium-derived growth factor (LEDGF)/p75 cofactor in lentiviral integration targeting. J Biol Chem (2011) 1.03
The thiazolobenzimidazole TBZE-029 inhibits enterovirus replication by targeting a short region immediately downstream from motif C in the nonstructural protein 2C. J Virol (2008) 1.02